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Herbimycin A (Antibiotic TAN 420F, (15R)-17-Demethoxy-15-methoxy-11-O-methyl-geldanamycin)
Benzoquinone ansamycin antibiotic. Herbicidal compound. Potent, selective, irreversible and cell permeable protein tyrosine kinase inhibitor. Inhibitor of v-Src, Yes, Fps, Ros, Bcr-Abl and ErbB oncogene products. Antitumor compound. Antiangiogenic. Inhibits NF-kappaB activation and phosphorylation of phospholipase C-gamma1. Inhibitor of heat shock protein 90 (Hsp90). Binds Hsp90 and destabilizes client proteins leading to their ubiquitination and proteasomal degradation. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Neuroprotective. Antiparasitic, antischistosomal agent. Antiviral. Increase microtubules sensitivity to cold in plants. Group: Biochemicals. Grades: Highly Purified. CAS No. 70563-58-5. Pack Sizes: 100ug, 1mg. Molecular Formula: C30H42N2O9. US Biological Life Sciences.
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Herg Activator (NS1643, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, Human ether-a-go-go related gene (hERG) K+ channel activator, KV11.1 Channel Activator)
A diphenolurea compound that selectively activates human ether-a-go-go-related gene (hERG) K+-channel (EC50=10.5uM). Shown to significantly increase both steady-state and peak tail currents of hERG channels, but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration (APD90) in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiamyocyes that can be reversed by the addition of E-4031, a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. It can also restore IKr reduced by down-regulation of IKr expression. Group: Biochemicals. Grades: Highly Purified. CAS No. 448895-37-2. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O?, Molecular Weight: 380.2. US Biological Life Sciences.
A potent agonist selective for u opioid receptor (Ki = 45nM) over kappa opioid receptors (Ki = 184nM). Widely used for pain research. Group: Biochemicals. Grades: Highly Purified. CAS No. 862073-77-6. Pack Sizes: 1mg. Molecular Formula: C??H??O?. US Biological Life Sciences.
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Hexacyclinic acid
Antibiotic and antitumor compound. Shows weak cytotoxicity against different tumor cell lines. Group: Biochemicals. Grades: Highly Purified. CAS No. 309757-85-5. Pack Sizes: 1mg. US Biological Life Sciences.
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Hexadecane
Hexadecane has been used to prepare emulsions in water. It is also used as a substrate for the bacterial production of biosurfactants. Group: Biochemicals. Grades: Highly Purified. CAS No. 544-76-3. Pack Sizes: 100mL, 500mL. Molecular Formula: C16H34, Molecular Weight: 226.44. US Biological Life Sciences.
A potent antagonist of nicotinic acetylcholine receptors (nAChRs) at pre-ganglionic sites in both the sympathetic and parasympathetic nervous systems. Often used for studying the roles of nicotinic receptors in regulating cardiovascular system. Group: Biochemicals. Grades: Highly Purified. CAS No. 55-97-0. Pack Sizes: 5g. Molecular Formula: C??H??Br?N?. US Biological Life Sciences.
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Hexen-5-ol
Hexen-5-ol is an intermediate in he synthesis of 5-Chloro-1-hexene which is a reagent with difluoroacetic acid that results in the formation of 5-chloro-2-hexyl-2-d trifluoro-acetate and 1,4-chlorine shift. Group: Biochemicals. Grades: Highly Purified. CAS No. 626-94-8. Pack Sizes: 50mg, 100mg. Molecular Formula: C6H12O. US Biological Life Sciences.
A cell-permeable acylguanidine compound that is shown to block Hh signaling and act as a potent, reversible and high-affinity Smo (Smoothened) antagonist. Displays 20-60 -fold greater potency than Cyclopamine and competitively inhibits bodipy-cyclopamine binding to Smo (IC50 = 4.6 and 14nM in HEK293-hSMO and HEK293-mSMO cells, respectively). Represses ShhN (N-myristoylated Shh) signaling (IC50=15nM for Gli-dependent luciferase activity in Shh-light2 cells) and SAG- induced C3H10T1/2 cell differentiation (IC50=10nM in an alkaline phosphatase activity assay). Inhibits ShhN (3nM) and SAG (10nM)-mediated proliferation of rat cerebellar granule cell precursors (IC50 ~3 and 6nM, respectively). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
A cell-permeable phenoxyacrylamido compound that inhibits hypoxia-induced cellular HIF-1alpha accumulation in a manner similar to LW6 by upregulating Hippel-Lindau tumor suppressor gene product pVHL, but with much higher potency (IC50 = 120nM vs 2.44uM, respectively, against hypoxia-induced HRE reporter activity in HCT116 cells). Shown to suppress HIF-1 target genes expression in HCT116 cultures and inhibit HUVEC tubule formation (effective conc. ≥2uM) under hypoxia conditions. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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HIF Inhibitor VII (Hypoxia-Inducible Factor Inhibitor VI, N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1, 2, 5]oxadiazol-5-amine)
A cell-permeable benzoxadiazolamine that prevents HIF-2alpha-HIF-beta/ARNT heterodimeration by perturbing HIF-2alpha Per-ARNT-Sim/PAS-B domain surface beta-sheet conformation via a 1:1 stoichiometric binding (KD = 81nM), while exhibiting no affinity toward HIF-1alphaPAS-B domain. Shown to be metabolically stable and non-cytotoxic in cultures and selectively inhibit hypoxia-induced HIF-2a DNA binding and HIF-2alpha-dependent EPO mRNA upregulation (1 to10uM for 6-12h), but not HIF-1alpha DNA binding or HIF-1alpha-dependent PGK1 mRNA upregulation, in Hep3B cells. Unlike HIF Inhibitors I-VI, this compound does not affect the cellular protein or mRNA levels of HIF-1alpha & HIF-2alpha. Group: Biochemicals. Grades: Highly Purified. CAS No. 1422955-31-4. Pack Sizes: 10mg. Molecular Formula: C??H?ClFN?O?, Molecular Weight: 308.65. US Biological Life Sciences.
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HIF-PHD Inhibitor II, JNJ-42041935 (HIF Prolyl Hydroxylase Inhibitor II, 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic Acid)
A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi=7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1a levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100uM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H?ClF?N?O?, Molecular Weight: 346.7. US Biological Life Sciences.
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Histone Acetyltransferase Inhibitor VIII, NU9056 (1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I, HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V)
A cell-permeable disulfane compound that is reported to be more potent against KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100uM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not alpha-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10uM). Shown to induce cell cycle arrest and apoptosis (17 to 24uM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C?H?N?S?, Primary Target: KAT5. US Biological Life Sciences.
A cell-permeable iron chelating benzisothiazolone compound with microbicide and fungicide properties that acts as a potent, selective, and reversible inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases (IC50 = 3uM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC50 = 6, 4.9, and 28uM for JARID1A, JARID1C, and JMJD2E, respectively). However, it does affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B show a significant reduction in H3K4Me3 activity following PBIT treatment (~10uM). Blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. Molecular Formula: C??H??NOS, Primary Target: JARID1 Histone Demethylases. US Biological Life Sciences.
A pyridinyl -pyrimidinyl aminopropanoic acid that effectively inhibits KDM6 family H3K27m3 demethylases JMJD3 and UTX (IC50 = 18 and 56uM, respectively, by MALDI Mass detection) in an alpha-ketoglutarate-competitive, peptide substrate-non-competitive manner, displaying much reduced potency against JARID1C, JMJD1a, JMJD2a, JMJD2c, JMJD2d, JMJD2e, as well as112 kinases and 60 non-kinase enzymes. Recommended for cell-free assays only. For culture treatment, use the cell-permeable pro-drug GSK-J4. Group: Biochemicals. Grades: Highly Purified. CAS No. 1373422-53-7. Pack Sizes: 10mg. US Biological Life Sciences.
A cell-permeable GSK-J1 prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50uM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-alpha production in primary human macrophage cultures (IC50 = 9uM by ELISA). Group: Biochemicals. Grades: Highly Purified. CAS No. 1373423-53-0. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?, Primary Target: H3K27me3 demethylases JMJD3 & UTX. US Biological Life Sciences.
A cell-permeable compound that is shown (at 1uM concentrations) to inhibit EZH2-mediated trimethylation of K27 on histone H3 and induces the expression of cell-cycle regulatory genes, p21 and p27, as well as the cell death regulator, FBXO32, in OCI-AML3 and HL-60 cells, whereby treatment with inhibitor increases p16 levels in the former, but not the latter of the two cultures. At concentrations between 200nM and 2000nM, this compound is found to dose-dependently deplete the expression of polycomb group proteins EZH2, SUZ12, and EED in cultured and primary AML cell extracts. At concentrations up to ≥ 1000nM, DZNep dose-dependently increases the percentage of apoptotic cells up to > ~ 38%, with greater potency against OCI-AML3 than HL-60 cultures and inhibits colony growth up to > ~ 85% for both cell lines. In OCI-AML3 cultures, 1000nM of treatment demonstrates a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of c Group: Biochemicals. Grades: Highly Purified. CAS No. 102052-95-9. Pack Sizes: 2mg. Molecular Formula: C??H??N?O?; HCl; H?O. US Biological Life Sciences.
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HMTase Inhibitor IV, UNC0638 (2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine)
A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50=<15 and 19nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50=4.66uM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50>10uM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50=81nM; EC50=11.2uM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294. Also, affects the activities of adrenergic a1A, adrenergic a and muscarinicM2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <30% at 1uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 2mg. US Biological Life Sciences.
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HMTase Inhibitor IX, MM-102 (Histone Methyltransferase Inhibitor IX, MM102, (S) -N- (bis (4-Fluoro phenyl ) methy l )-1- (2- (2-ethyl -2-isobutyramidobutanamid o)-5-guanidinopentanamido) cyclopentane carboxami de , TFA)
A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells (50uM for 96 h) and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25uM) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O? · CF?CO?H. US Biological Life Sciences.
A cell-permeable analog of the amino-benzimidazolo BIX-01338 and the methylester prodrug of BRD9539 that acts as an SAM-competitive inhibitor against PRC2 and G9a (IC50<6.3uM) histone methyltransferase activities, displaying little effect toward 10 other HMTases, 9 HDACs, and 100 cellular kinases. Selectively reduces H3K9me2 and H3K9me3 (EC50=5uM) histone methylation levels in pancreatic cancer cells (PANC-1) with much less or little effect toward H3K36me3, H3K4me3, H3K27me3, or H3K6me3 levels. Inhibits both anchorage-dependent and -independent PANC-1 proliferation via ATM activation and G2/M cell-cycle arrest, but not apoptosis induction (no caspase3/7 activation; 10uM, 72h). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
A quinazolinamine compound that acts as a potent, reversible and SAM (S-adenosylmethionine) non-competitive inhibitor of methyltransferases G9a (H3K9 HMT/EHMT2; IC50=15nM; =23nM) and GLP (G9a-like protein/EHMT1; IC50=20nM). Displays 1,000-fold greater selectivity for G9a over SET7/9 (H3K4 HMTase), SET8/PreSET7 (H4K20 HMTase), PRMT3 (MTase) and JMJD2E (demethylase), and minimally affects the activities of a broad range of GPCRs, ion-channels and transporters in a 30-target selectivity panel, with the exception of muscarinic M2 receptor and histamine H1 receptors (82% and 31% inhibition at 1uM, respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 1197196-48-7. Pack Sizes: 5mg. US Biological Life Sciences.
A cell-permeable phenyl sulfonyl benzimidazole that is shown to dock in the ligand-binding pocket of both HNF4a and HNF4g and antagonize HNF4a DNA binding activity in HepG2 cells (by 93%; 10uM overnight), effectively inhibiting HNF4a-dependent cellular activities (Effective conc. 1 to 5uM). HNF4g inhibition by BI6015 can also lead to decreased insulin promoter binding by transactivators E47 & PDX-1 in T6PNE cells (5uM 48h). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10uM), but not primary murine hepatocytes, it does cause hepatic steatosis both in vitro and in mice in vivo, limiting its use in animal studies. BI6015 also inhibits Human CYP450 2C19 and rat L-type calcium channel (by 94% and 83%, respectively, at 10uM), but not PPARg or a panel of 41 receptors/enzymes of human, mouse, and rat origin. Group: Biochemicals. Grades: Highly Purified. CAS No. 93987-29-2. Pack Sizes: 25mg. Molecular Formula: C??H??N?O?S, Molecular Weight: 331.4. US Biological Life Sciences.
A potent agonist fornMDA receptor with subunit-selectivity of NR2A/B (EC50 = 26uM) over NR2C (EC50 = 60uM). Used as a potent neurotoxic agent and for identifying endogenous receptors containing the NR2C subunit. Group: Biochemicals. Grades: Highly Purified. CAS No. 490-75-5. Pack Sizes: 10mg. US Biological Life Sciences.
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HSP70 Activator II, YM-08 ( (2Z, 5E) -3-ethyl-5- (3-methylbenzo[d]thiazol-2 (3H) -ylidene) -2- (pyridin-2-ylmethylene) thiazolidin-4-one, Heat Shock 70kD Protein Activator II, Hsp70 Chemical Co-Chaperone II, YM-08, YM08, YM8)
A cell-permeable, neutrally charged, pyridinium-to-pyridine substituted YM-01 and MKT-077 structural analog that exhibits higher HSP70-binding affinity, but reduced tau degradation-promoting potency in cultures (% degradation of p-tau/total tau = 42/64, 88/89, and 81/80 in HeLaC3 with 30uM YM-08, MKT-077, or YM-01, respectively) and weaker anti-cancer activity (IC50 against MDA-MB-231/MCF10A/MCF7 inuM = 1.4/3.0/2,2/MKT-077, 2.0/3.3/5.2/YM-01, and 8.5/7.8/10.5/YM-08 in 72h). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
Humulene
Humulene is a monocyclic sesquiterpene derived from farnesyl diphosphate and naturally found in clove, basil, hops, and cannabis sativa. Humulene has potential anti-inflammatory, anti-tumor, and anti-bacterial properties. Group: Biochemicals. Grades: Highly Purified. CAS No. 6753-98-6. Pack Sizes: 100mg, 250mg. Molecular Formula: C15H24. US Biological Life Sciences.
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Hydrobromic Acid Solution (in Acetic Acid)
Hydrobromic acid is a strong acid that is used in conjunction with Phenol (P318005) to carry out rapid cleavage of sulfonamides. Hydrobromic acid is also used as a catalyst to reduce sulfoxides, such as Dimethyl sulfoxide (D479380). Group: Biochemicals. Grades: Highly Purified. CAS No. 37348-16-6. Pack Sizes: 10ml, 25ml. Molecular Formula: HBr. US Biological Life Sciences.
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Hydromorphone
Hydromorphone provides a satisfactory analgesia for children with cerebral palsy surgery. Semisynthetic opioid receptor agonist. Also, it is an intermediate useful in the synthesis of Hydromorphone N-Oxide Hydrochloride (H714685), which is a metabolite of opiate analgesic, Hydromorphone (H714650). Group: Biochemicals. Grades: Highly Purified. CAS No. 466-99-9. Pack Sizes: 5mg, 10mg. Molecular Formula: C17H19NO3, Molecular Weight: 285.339999999999. US Biological Life Sciences.
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Hydroxypropyl-beta-cyclodextrin
Hydroxypropyl-beta-cyclodextrin. Group: Molecular Biology. CAS No. 128446-35-5. Pack Sizes: 25g, 100g. US Biological Life Sciences.
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Hydroxypropyl Chitosan
Hydroxypropyl Chitosan is an antibacterial used to make organic rectorite-based nanofibrous mats with bacterial inhibition. Hydroxypropyl Chitosanhas been shown to exhibit inhibitory effects on the levels of Fe, Zn and Ca in liver, heart, lung, spleen, kidney and femur at high dosages in mice. Group: Biochemicals. Grades: Highly Purified. CAS No. 84069-44-3. Pack Sizes: 100mg, 1g. Molecular Formula: [C16H33NO7]x. US Biological Life Sciences.
Displays a variety of biological activities including anti-bacterial, anti-inflammatory, anticancer and anti-angiogenic effects. Also acts as an antidepressant and anxiolytic agent. Regulates expression of the cytochrome P450 CYP3A4 and CYP2C9 and hepatic drugs metabolism. Inhibits the re-uptake of neurotransmitters in synapses (serotonin, norepinephrine, dopamine, GABA, glutamate). Also acts as a potent SIRT1 and SIRT2 inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 238074-03-8. Pack Sizes: 500ug, 1mg. US Biological Life Sciences.
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Hypothemycin
Antifungal. Cytotoxic against some tumor cell lines, partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells. Modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Potent and selective threonine/tyrosine-specific kinase, MEK and other protein kinases inhibitor in both in vitro and in vivo studies. Group: Biochemicals. Alternative Names: 3H-Oxireno [k] [2] benzoxacyclotetradecin-5, 11 (2H, 4H) -dione, 1a, 8, 9, 15b-tetrahydro-3, 4, 12-trihydroxy-14-methoxy-9-methyl-, (1aR, 3S, 4S, 6Z, 9S, 15bR) -, NSC354462. Grades: Highly Purified. CAS No. 76958-67-3. Pack Sizes: 250ug, 1mg. Molecular Formula: C??H??O?. US Biological Life Sciences.
A highly selective antagonist for the beta-2 adrenergic receptors. Binds to the beta-2 subtype with at least 100 times greater affinity than beta-1 or beta-3, the two other known subtypes of the beta adrenoceptor. (Ki values are 1.2, 120 and 257nM for beta-2, beta-1 and beta-3 receptors respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 72795-19-8. Pack Sizes: 10mg. US Biological Life Sciences.
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ICMT Inhibitor (Cysmethynil)
An inhibitor of protein prenylation. Cysmethynil is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT) with antitumor activity in cancer cells. Cysmethynil treatment results in inhibition of cell growth in an Icmt-dependent fashion, demonstrating mechanism-based activity of the compound. Treatment of cancer cells with cysmethynil results in mislocalization of Ras and impaired epidermal growth factor signaling. In a human colon cancer cell line, cysmethynil treatment blocks anchorage-independent growth, and this effect is reversed by overexpression of Icmt.A cell-permeable indole acetamide that acts as a substrate-competitive and AdoMet-noncompetitive Icmt...25uM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy. Group: Biochemicals. Alternative Names: Cysmethynil; 2-(5-(3-Methylphenyl)-1-octyl-1H-indol-3-yl)acetamide, 2-(1-Octyl-5-m-tolyl-1H-indol-3-yl) acetamide; Isoprenylcysteine Carboxyl Methyltransferase Inhibitor). Grades: Highly Purified. CAS No. 851636-83-4. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C25H32N2O, Molecular Weight: 376.5. US Biological Life Sciences.
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ICMT Inhibitor II, FTPAT ((E)-methyl-3-((5-(4-(2-((1,1-biphenyl]-4-yl)ethyl)-1H-1,2,3-triazol-1-yl)-3-methylpent-2-en-1-yl)thio)propanoate)
A cell-permeable triazolo-farnesylthiopropanoate compound that acts as a potent, reversible, and isoprenyl mimetic competitive inhibitor of isoprenylcysteine carboxyl methyltransferase activity (ICMT; IC50=800nM; Ki=400nM). Shown to prevent K-Ras membrane localization in GFP-K-Ras transfected Jurkat T-cells. Exhibits selective toxicity towards wt-Icmt+/+ mouse embryonic fibroblasts (MEFs) over Icmt-/- MEFs (IC50=33 and >100uM). Also shown to arrest the proliferation of PaTu-8902, a highly metastatic pancreatic cancer cells (IC50=8uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
A non-selective antagonist for alpha-2-adrenoceptors (pKi = 8.01, 7.43, and 7.7 for alpha-2A, alpha-2B, and alpha-2C receptors respectively) and imidazoline receptors. (pKi = 5.90, 7.22 for I1 and I2, receptors respectively). Widely used in studying functions of the nervous systems, such as learning and memory, decision making, reward, attention, addiction, depression, and schizophrenia related to the adrenergic receptors, and blood pressure regulation, pain modulation, and neuroprotection related to the imidazoline receptors. Group: Biochemicals. Grades: Highly Purified. CAS No. 79944-56-2. Pack Sizes: 50mg. US Biological Life Sciences.
Cell-permeable. Directs differentiation of embryonic stem cells (ESCs) into the endodermal lineage (EC??=125nm). Nodal/Smad signaling is activated indicating IDE-1 functions via TGF-b-signaling pathway. Group: Biochemicals. Grades: Highly Purified. CAS No. 1160927-48-9. Pack Sizes: 1mg, 5mg . US Biological Life Sciences.
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IDS, Positive Control (Iduronate-2-Sulfatase, Alpha-L-iduronate Sulfate Sulfatase, Idursulfase, SIDS)
IDS, Positive Control (Iduronate-2-Sulfatase, Alpha-L-iduronate Sulfate Sulfatase, Idursulfase, SIDS). Group: Molecular Biology. Pack Sizes: 15ul. US Biological Life Sciences.
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Ifenprodil
Ifenprodil is a NMDA receptor antagonist. Group: Biochemicals. Grades: Highly Purified. CAS No. 23210-56-2. Pack Sizes: 5mg, 10mg. Molecular Formula: C21H27NO2, Molecular Weight: 325.44. US Biological Life Sciences.
A partial non-competitive antagonist highly selective for GluN1/N2B subtype nMDA receptors (IC50 = 0.15uM, maximal inhibition 90%) over other subtypes (IC50 = 39, 29, 76uM for GluN1/N2A, GluN1/N2C and GluN1/N2D subtype receptors, respectively). Frequently used in studies of various brain functions and disorders involving neural transmissions mediated by GluN1/N2B subtype nMDA receptors. Group: Biochemicals. Grades: Highly Purified. CAS No. 23210-58-4. Pack Sizes: 10mg. US Biological Life Sciences.
A cell-permeable BX795 analog that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKK epsilon (IC50 = 19 and 160nM, respectively) with excellent selectivity over IKKalpha and IKKbeta (IC50 > 10uM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC50 = 27, 52, 36, and 41nM, respectively), SIK2 (IC50 = 67nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1uM) in a 108-kinase panel. Increases TNF-alpha-stimulated NF-kB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflamm Group: Biochemicals. Grades: Highly Purified. CAS No. 495-85-2. Pack Sizes: 5mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences.
A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50=600nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50=1 to 2.5uM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C30H30F3N5O, Molecular Weight: 553.6. US Biological Life Sciences.
Worldwide
Imatinib, Free base
An inhibitor of the bcr-abl tyrosine kinase. It acts by binding to the ATP binding site of bcr-abl. Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. It inhibits EOL-1 cell viability (IC50=0.5nm), phosphorylation of a fusion protein (IC50=30nm), and viability of BaF3 cells expressing Rhe-PDGFRa in the absence of IL-3 (IC50 =0.17nm). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 100ug, 1g. US Biological Life Sciences.
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Imipenem, δ1
Imipenem, δ1. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg. Molecular Formula: C12H17N3O4S, Molecular Weight: 299.35. US Biological Life Sciences.
A furanocoumarin isolated from Opopanax chironium L. Displays anticancer properties. It induces apoptosis as well as DNA fragmentation at the G1/S phase of the cell cycle. Imperatorin sensitizes anoikis and inhibits anchorage-independent growth of lung cancer cells. Modulator of SMAD1/5/8, p38, ERK pathways. Also acts as a L-type calcium channel blocker. Group: Biochemicals. Alternative Names: 9-(3-methylbut-2-enoxy)furo[3,2-g]chromen-7-one. Grades: Highly Purified. CAS No. 482-44-0. Pack Sizes: 5mg, 25mg. US Biological Life Sciences.
A cell-permeable diaminoquinazoline compound that selectively blocks importin-b-mediated nuclear import of NLS- (nuclear localization signal) bearing cargos (IC50=15uM against Ca+2-induced NFAT nuclear import in HEK293 cells) in a reversible manner without affecting transportin-dependent nuclear import of M9 signal-containing cargos or CRM1-mediated nuclear export. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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(-)-Indolactam V ((2S,5S)-1,2,4,5,6,8-Hexahydro-5-(hydroxymethyl)-1-methyl-2-(1-methylethyl)-3H-pyrrolo[4,3,2-gh]-1,4-benzodiazonin-3-one)
Cell-permeable. A protein kinase C (PKC) activator and a tumor promoter. Directs differentiation of human embryonic stem cells (ESCs) into pancreatic progenitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 90365-57-4. Pack Sizes: 250ug, 1mg. US Biological Life Sciences.
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Indole-3-propionamide
Indole-3-propionamide is a novel endogenous indole derivative which has a similar structure to melatonin. It acts as a stabilizer of energy metabolism, thereby reducing reactive oxygen species (ROS) production. Group: Biochemicals. Grades: Highly Purified. CAS No. 5814-93-7. Pack Sizes: 100mg, 250mg. Molecular Formula: C11H12N2O, Molecular Weight: 188.23. US Biological Life Sciences.
A cell-permeable, bioavailable 2-trifluoromethyl analog of Indomethacin that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2; IC50=267 and 388nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC50 >100uM). Interacts with human COX-2 with much greater affinity than indomethacin (KI = 1.5 vs 13uM) and blocks COX-2 dependent arachidonic acid oxygenation (IC50 = 150nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC50 = 1.7mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10mg/kg). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
A cell-permeable, hexapeptide containing a novel integrin-binding motif, SDV (a Type I PDZ-binding motif) that is shown to compete with vitronectin for the RGD-binding site of integrin avb3 (IC50=1.74pg/ml), in a chip-based assay. It is rapidly internalized into HUVECs, but not in NIH 3T3 cells, at a culture temperature of 37°C, a process which is mediated by caveolin and clathrin. At 10u/ml, this compound is shown to significantly inhibit the phosphorylation of ERK1/2 and MEK in HUVECs. Furthermore, it suppresses bFGF-induced proliferation of HUVECs, dose-dependently, and displays up-regulation of p53 and induction of apoptosis via activation of caspases-3, -8 and -9 at 50ug/ml. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
A nonpeptidic thiophenylmethanamine compound that binds interferon-a (Kd= 4uM for human IFN-a) and prevents IFN-a and IFNAR interaction-dependent IFN-a production in murine BM-pDCs (bone marrow-derived plasmacytoid dendritic cells) cultures upon MVA infection (IC50<4.5uM), while exhibiting no inhibitory effect against IL-12 production in the same cultures when applied at non-toxic concentrations (<4.5uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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Ionomycin (Free Acid)
Antibiotic. Potent and highly selective Ca2+ ionophore. Commonly used to modify intracellular calcium levels to study calcium transport across biological membranes and to calibrate fluorescent Ca2+ indicators. Ionomycin also transports Pb2+ and some other divalent cations, as well as several lanthanide series trivalent cations at efficiencies that are greater than or equal to those for Ca2+. Apoptosis inducer. Induces apoptotic neuronal degeneration in embryonic cortical neurons and cell cycle arrest at G1 phase and induces central demyelination. Used to stimulate the intracellular production of the cytokines, interferon, perforin, IL-2 and IL-4 usually in conjunction with PMA. ADAM10 agonist. Potent inducer of shedding CXCL16. TREK-1 channels inhibitor. PPARy ligand with a unique binding mode. Shows effective glucose-lowering activity in a mouse model of diabetes. Group: Biochemicals. Alternative Names: SQ 23377; EM 94; [2S-[2α[2S*, 5R*(S*)], 5 β(4S*, 6R*, 8R*, 10Z, 12S*, 14S*, 16E, 18S*, 19S*, 20R*, 21R*)]]-11, 19, 21-Trihydroxy-4, 6, 8, 12, 14, 18, 20-heptamethyl-22-[octahydro-5-(1-hydroxyethyl)-2, 5-dimethyl[2, 2-bifuran]-5-yl]-9-oxo-10, 16-docosadienoic Acid; [2S-[2α[2S*, 5R*(S*)], 5 β(4S*, 6R*, 8R*,. Grades: Highly Purified. CAS No. 56092-81-0. Pack Sizes: 1mg, 5mg. Molecular Formula: C??H??O?. US Biological Life Sciences.
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iPSC Induction Enhancer II, OAC1 N-(1H-Pyrrolo[2,3-c]pyridin-5-yl)benzamide, Induced Pluripotent Stem Cells Induction Enhancer II, Oct4-Activating Compound 1)
A cell-permeable pyrrolopyridinyl-benzamide compound that is reported to enhance the efficiency of 4F/4TF-induced iPSC generation from MEFs cultured in either feeder cell-containing ESC media or in feeder-/serum-free iSF1 media (1uM OAC1 treatment starts 48h after viral transduction). OCA1 is shown to increase cellular Oct4, Nanog, Sox2, and Tet1 mRNA levels via a yet unidentified mechanism, although OAC1 is reported not affect Oct4 promoter methylation, cellular Wnt signaling, or p53 and p21 mRNA levels. Six other iPSC reprogramming improving reagents, AM580, AzaC, BIX-01294, Tranylcypromine, VPA, and Vitamin C, in comparison, do not exhibit Oct4 and Nanog promoters enhancing activity, while BIO is demonstrated to be 3.8- and 6-fold less potent than OAC1, respectively, in inducing Oct4 and Nanog transcription. Group: Biochemicals. Grades: Highly Purified. CAS No. 300586-90-7. Pack Sizes: 25mg. Molecular Formula: C??H??N?O, Molecular Weight: 237.3. US Biological Life Sciences.
A cell-permeable aminothiazolo-carboxamide compound that is reported to augment SB431542 and PD0325901 in enhancing human iPSCs (induced Pluripotent Stem Cells) generation from fibroblast cultures virally transfected with 4-TF (Oct44, Klf4, Sox2, and c-Myc). Simultaneous blockage of TGFb and MEK-ERK pathways by SB431542 (2uM) and PD0325901 (0.5uM) in addition to 4-TF-induction is shown to result in >50-fold improvement of iPSCs generation, while the inclusion of Thiazovivin (0.5uM) on top of SB431542 and PD0325901 is demonstrated to further improve the efficiency to an over-all of >200-fold improvement from 4-TF-induction alone. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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IRE1 Inhibitor III, 4u8C (8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde, ER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III)
A cell-permeable coumarin o-hydroxyaldehyde that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50=550 and 45nM, respectively, with 0 and 16min drug preincubation in RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50=6.9 and 4.1uM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin treatment. Comparing to STF083010, 4u8C is also shown to inhibit IRE1 autophosphorylation in cell-free assays via Schiff base formation with IRE1 Lys599 in the absence of ADP, however cellular nucleotide prevents 4u8C from targeting IRE1 Lys599 intracellularly. Group: Biochemicals. Grades: Highly Purified. CAS No. 14003-96-4. Pack Sizes: 25mg. US Biological Life Sciences.
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Iromycin A
Pyridone metabolite. Nitric oxide synthase (NOS) inhibitor, showing selectivity for eNOS (NOS III) versus nNOS (NOS I). Thaxtomine biosynthesis inhibitor and mitochondrial electron transport chain inhibitor.CAS Number:213137-53-2. Group: Biochemicals. Grades: Highly Purified. CAS No. 213137-53-2. Pack Sizes: 500ug, 1mg. US Biological Life Sciences.
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Iron Chelator IV, 21H7 (6-Bromo-N-(2-hydroxybenzylidene)-2-methylquinoline-4-carbohydrazide)
A cell-permeable salicylaldehyde-acylhydrazone iron chelator that is 20-times more efficient than DFO/desferrioxamine in depleting intracellular iron in colon cancer SW480 cells. Iron chelators exert their biological activities by affecting iron-regulated enzymes and singaling events, including HIF1a transcription activation due to inhibition of PHD- (prolyl hydroxylase) mediated HIF1a degradation, as well as altered mRNA translations due to enhanced IRP (Iron Regulatory Protein) IREs (Iron Response Elements) binding. Cellular iron depletion is also reported to inhibit the growths of colorectal adenocarcinoma cultures, DLD-1 (IC50=0.6 and 2.9uM, respectively, by 21H7 and DFO) and SW480 (IC50=1.0 and 3.8uM, respectively, by 21H7 and DFO), as a result of Wnt signaling pathway blockage (Effective conc.=5uM 21H7 or 100uM DFO). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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Iron(III) Chloride
Iron(III) Chloride is commonly employed as a Lewis acid for catalysing reactions such as chlorination of aromatic compounds and Friedel-Crafts reaction of aromatics. In industrial application, iron(III) chloride is used in sewage treatment and drinking water production. It is also used as a leaching agent in chloride hydrometallurgy. Group: Biochemicals. Grades: Highly Purified. CAS No. 7705-08-0. Pack Sizes: 10g, 25g. Molecular Formula: Cl3Fe, Molecular Weight: 162.199999999999. US Biological Life Sciences.
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IRTK Activator III, DDN (5,8-Diacetyloxy-2,3-dichloro-1,4-naphthoquino)
An orally bioavilable diacetyloxy-naphthoquinone compound that directly targets insulin receptor tyrosine kinase (IRTK) domain and specifically increases IR kinase activity with no effect on IGF-1R and EGFR. Shown to rapidly phosphorylate IR (Tyr1146 and Tyr1158/1162/1163) and IRS-1 and selectively activate insulin signaling Akt (Thr473) and ERK pathways in CHO-IGF-IR cells at 5uM. Sensitizes insulin action, enhances glucose uptake in differentiated 3T3-L1 adipocytes and decreases blood glucose levels in both normal and diabetic C57BL/6J mice (20mg/kg, p.o.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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Isatropolone A
Antileishmanial agent. Active against Leishmania donovani, the causative agent of visceral leishmaniasis. Showed no activity against intracellular Leishmania. Isatropolone A is an. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
A cell-permeable azobenzene compound that reversibly targets CREB-binding protein bromodomain (CBP-BRD) acetyl-lysine binding pocket (=19uM) with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B ( = 37, 41, 70 and >100uM, respectively) and disrupts CBP interaction with the binding partners. Blocks CBP-p53 interaction and alters the post-translational modification states on p53 and histones. Shown to inhibit the transcription functions of p53 on DNA damage (IC50=5uM for p53-induced p21 activation in Luc-U2OS cells) and suppress cardiac myocyte apoptosis during ischemia conditions. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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Isodecyl Methacrylate
Isodecyl Methacrylate is a reagent used in the preparation of Janus particles which act as solid surfactants. Group: Biochemicals. Grades: Highly Purified. CAS No. 29964-84-9. Pack Sizes: 1g, 5g. Molecular Formula: N/A, Molecular Weight: US Biological Life Sciences.
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Isofusidienol A
Antibiotic and chromone derivative. Antifungal and antibacterial against Gram-positive and Gram-negative bacteria. Group: Biochemicals. Alternative Names: Methyl-10-hydroxy-8-methyl-11-oxo-11H-oxepino[4,5-b]chromene-1-carboxylate. Grades: Highly Purified. CAS No. 1032392-18-9. Pack Sizes: 1mg. Molecular Formula: C16H12O6. US Biological Life Sciences.
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Isophorone Diisocyanate
Isophorone Diisocyanate is a reagent used in the synthesis f an epoxy monomer from 2,5-Furandimethanol. Group: Biochemicals. Grades: Highly Purified. CAS No. 4098-71-9. Pack Sizes: 10ml, 50ml. Molecular Formula: C12H18N2O2, Molecular Weight: 222.28. US Biological Life Sciences.
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Isosafrole
Isosafrole, can be used in fragrance industry, as it has fragrance reminiscent of anise or licorice. It is a precursor to the important fragrance Piperonal (P490050). It can also be used as an intermediate for the synthesis of psychoactive drug MDMA (M303985). Group: Biochemicals. Grades: Highly Purified. CAS No. 120-58-1. Pack Sizes: 250mg, 2.5g. Molecular Formula: C10H10O2, Molecular Weight: 426.5. US Biological Life Sciences.
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Isovaleric acid
Isovaleric acid (I917570) is a naturally occurring aroma compound found in Bartlett pear brandies, vanilla beans, rape-honey and banana. Group: Biochemicals. Grades: Highly Purified. CAS No. 503-74-2. Pack Sizes: 100g, 250 g. Molecular Formula: C5H10O2. US Biological Life Sciences.
Worldwide
Itaconic acid
Inhibitor of isocitrate lyase, the key enzyme of the glyoxylate cycle, essential for bacterial growth. Antimicrobial. Antibacterial. Inhibits the growth of bacteria expressing isocitrate lyase. Phosphofructokinase (PFKII) inhibitor. Suppresses glycolysis by decreasing the level of fructose 2,6-bisphosphate, resulting in decreased visceral fat. Might be involved in the regulation of metabolism. Group: Biochemicals. Alternative Names: 2-Methylenebutanedioic Acid; Methylenesuccinic Acid; 2-Methylenebutanedioic Acid; 2-Methylenesuccinic Acid; 2-Propene-1,2-dicarboxylic Acid; 4-Hydroxy-2-methylene-4-oxobutanoic Acid; Methylenebutanedioic Acid; NSC 3357; Propylenedicarboxylic Acid. Grades: Highly Purified. CAS No. 97-65-4. Pack Sizes: 1g, 5g. Molecular Formula: C?H?O?. US Biological Life Sciences.
Cell-permeable. ITSA-1 is a suppressor of Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct acetylation events (histone and tubulin). ITSA-1 specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 reverses TSA induced histone acetylation, overall deacetylation. ITSA-1 also reverses TSA induced cell cycle arrest and apoptosis. Group: Biochemicals. Grades: Highly Purified. CAS No. 200626-61-5. Pack Sizes: 5mg. US Biological Life Sciences.
Cell-permeable. Acts as an inhibitor of Wnt secretion and processing. It blocks Wnt-dependent signaling (IC50 = 27nM) by inhibition of the O-acyltransferase Porcn. Porcn is a member of the membrane-bound O-acyltransferase (MBOAT) family, which adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 25mg. US Biological Life Sciences.
A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3b, JAK3, PKCa and PKCth (IC50=3, 8, 13 and 68nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50=1.017, 2.55 and 8.055uM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50=0.525, 1.294 and 0.689uM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 1260181-14-3. Pack Sizes: 5mg. Molecular Formula: C??H??F?N?O?, Molecular Weight: 526.5. US Biological Life Sciences.
A cell-permeable steroidal-purinethione that targets JAK3 kinase domain and selectively inhibits JAK3, but not JAK1, JAK2, or TYK2, activity and effectively blocks the constitutive Jak3 and STAT5 phosphorylations (complete inhibition at 10uM) in BaF3-JAK3V674A and BLNK-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3WT, BaF3-JAK3V674A, and BLNK-/- BKO84 cells (by 40%, 50%, 57%, and 85%, respectively; 20uM; 72 h), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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JAK Inhibitor I (P6, DBI, (2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, JAK1 Inhibitor I, JAK3 Inhibitor VII, JAK2 Inhibitor I)
A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50=15nM for murine JAK1), JAK2 (IC50=1nM), JAK3 (Ki=5nM), and Tyk2 (IC50=1nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490. A 10mM solution of JAK Inhibitor I in DMSO is also available. Group: Biochemicals. Grades: Highly Purified. CAS No. 457081-03-7. Pack Sizes: 500ug, 1mg. US Biological Life Sciences.