BOC Sciences provides a wide range of research chemicals and biochemicals including inhibitors, building blocks, GMP Products, impurities and metabolites, APIs for Veterinary, Natural Compounds, ADCs, Stem Cell Molecule and chiral compounds.
| Product | Description | |
|---|---|---|
| CAY10444 | CAY10444 is a family of related G-protein coupled receptors that bind sphingosine-1 phosphate (S1P) as a high-affinity ligand have recently been cloned. It is a selective antagonist of S1P binding to the S1P3 receptor, blocking the calcium increase in HeLa cells by about 40% when present at 10 μM. Synonyms: BML-241; CAY 10444; CAY-10444; BML 241. Grade: ≥98%. CAS No. 298186-80-8. Molecular formula: C15H29NO2S. Mole weight: 287.5. |  |
| CAY10448 | Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel. It is also an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of 10 nM. Synonyms: CAY 10448; CAY-10448. Grade: ≥98%. CAS No. 1177195-52-6. Molecular formula: C18H28INO3. Mole weight: 433.3. | |
| CAY10449 | CAY10449 is one of compounds which are found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor. It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase. It also inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 3 nM. Synonyms: CAY 10449; CAY-10449. Grade: ≥98%. Molecular formula: C19H21N3O2. Mole weight: 323.4. | |
| CAY10462 | 20-HETE is an important metabolite of arachidonic acid in the vasculature, especially in the kidney, where it is synthesized by cytochrome P450 (CYP450) enzymes of the 4A family. CAY10462 is the hydrochloride salt form of CAY10434. It is a selective inhibitor of the 20-HETE synthase CYP4A11, which exhibits an IC50 of 8.8 nM when tested in human renal microsomes. Synonyms: CAY 10462; CAY-10462. Grade: ≥98%. CAS No. 502656-68-0. Molecular formula: C17H25N3O·2HCl. Mole weight: 360.3. | |
| CAY10464 | The aryl hydrocarbon receptor (AHR) is a ligand-dependent intracellular transcription factor whose ligands include some of the most infamous xenobiotics. CAY10464 is a potent and selective AhR antagonist with a Ki of 1.4 nM. It is inactive as an estrogen receptor ligands even used at 100 μM. Synonyms: CAY 10464; CAY-10464. Grade: ≥98%. CAS No. 688348-37-0. Molecular formula: C15H12Cl2O. Mole weight: 279.2. | |
| CAY10465 | The aryl hydrocarbon receptor (AHR) is a ligand-dependent intracellular transcription factor. CAY10465 is an analog of resveratrol which acts as a potent and selective AHR receptor agonist with Ki of 0.2 nM. It is inactive as a ligand for the estrogen receptor. Synonyms: CAY 10465; CAY-10465. Grade: ≥98%. CAS No. 688348-33-6. Molecular formula: C15H9Cl2F3. Mole weight: 317.1. | |
| CAY10471 | CAY10471 is an analog of BAY-u3405, which contains modifications that increase both its potency and selectivity for the human CRTH2/DP2 receptor. CAY10471 binds to the human DP1 with Ki of 1200 nM and DP2 with Ki of 0.6 nM. It also show very high binding affinity with TP, which Ki can higher than 10,000 nM. Synonyms: CAY-10471; CAY 10471; TM-30089; TM 30089. Grade: ≥95%. CAS No. 627865-18-3. Molecular formula: C21H21FN2O4S. Mole weight: 416.5. | |
| CAY10485 | Acetyl-CoA acetyltransferase, mitochondrial, also known as acetoacetyl-CoA thiolase, is an enzyme that in humans is encoded by the ACAT (Acetyl-Coenzyme A acetyltransferase) gene. Both ACAT-1 and ACAT-2 are acetyl-CoA C-acetyltransferase enzyme. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins. Synonyms: 3,4-dihydroxy Hydrocinnamic acid (L-Aspartic acid dibenzyl ester) amide. Grade: ≥98%. CAS No. 615264-62-5. Molecular formula: C27H27NO7. Mole weight: 477.5. | |
| CAY10486 | Acetyl-CoA acetyltransferase, mitochondrial, also known as acetoacetyl-CoA thiolase, is an enzyme that in humans is encoded by the ACAT (Acetyl-Coenzyme A acetyltransferase) gene. Both ACAT-1 and ACAT-2 are acetyl-CoA C-acetyltransferase enzyme. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins. Synonyms: 4-Hydroxycinnamic acid (L-phenylalanine methyl ester) amide. Grade: ≥98%. CAS No. 615264-52-3. Molecular formula: C19H19NO4. Mole weight: 325.4. | |
| CAY10498 | The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective Adenosine A3-R (A3 AR) antagonist exhibiting a Ki of 37 nM. It is 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, which is a dedifferentiation agent of embryonic progenitor cells. Synonyms: 2-phenyl-amino-N6-endo-norbornyladenine. Grade: ≥95%. CAS No. 863202-33-9. Molecular formula: C18H20N6. Mole weight: 320.4. | |
| CAY10499 | Monoglyceride lipase (MGL) plays an important role in the metabolism of the lipid transmitter 2-arachidonoylglycerol (2-AG). CAY10499 is a potent and selective monoglyceride lipase (MGL) inhibitor exhibiting an IC50 of 90 nM for the recombinant enzyme. It is also a non-selective lipase inhibitor (IC50s = 144, 90, and 14 nM for human recombinant MAGL, HSL, and FAAH, respectively). CAY10499 inhibits the growth of MCF-7, MDA-MB-231, COV318, and OVCAR-3 cancer cells (IC50s = 4.2, 46, 106.7, and 79.8 mM, respectively). Synonyms: CAY-10499; CAY 10499; Magl-IN-5. Grade: ≥98%. CAS No. 359714-55-9. Molecular formula: C18H17N3O5. Mole weight: 355.34. | |
| CAY10502 | Phospholipases A2 (PLA2s) are enzymes that cleave fatty acid in position two of phospholipids, hydrolyzing the bond between the second fatty acid "tail" and the glycerol molecule. It catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. CAY10502 is a potent Calcium-dependent cytosolic PLA2 (cPLA2α) inhibitor with IC50 value of 4.3 nM for the purified enzyme from human platelets. It inhibits arachidonic acid mobilization from A23187-stimulated or TPA-stimulated human platelets with IC50 values of 570 and 0.9 nM, respectively. Synonyms: CAY10502; CAY-10502. Grade: ≥98% (mixture of isomers). CAS No. 888320-29-4. Molecular formula: C30H37NO7. Mole weight: 523.6. | |
| CAY10505 | CAY10505 is a phosphatidylinositol 3-kinase-γ inhibitor, was found to significantly improve acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. CAY10505, may improve hypertension-associated vascular endothelial dysfunction. Inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction. Synonyms: CAY10505; CAY 10505; CAY-10505. Grade: 0.98. CAS No. 1218777-13-9. Molecular formula: C14H8FNO3S. Mole weight: 289.28. | |
| CAY10506 | Peroxisome proliferator-activated receptor gamma (PPARγ), also known as the glitazone receptor, or NR1C3, is a type II nuclear receptor that in humans is encoded by the PPARG gene. CAY10506 is a PPARγ agonist, which is a nuclear transcription factor that controls lipid homeostasis and glucose metabolism. It is a hybrid lipoic acid (anti-diabetic drugs of the thiazolidinedione) TZD derivative that transactivates human PPARγ with an EC50 value of 10 μM. Synonyms: CAY 10506; CAY-10506. Grade: ≥98%. CAS No. 292615-75-9. Molecular formula: C20H26N2O4S3. Mole weight: 454.6. | |
| CAY10508 | Cannabinoid receptor type 1 (CB1) is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM. Synonyms: CAY 10508; CAY-10508. Grade: ≥98%. CAS No. 878533-35-8. Molecular formula: C21H14Br2N2O2. Mole weight: 486.2. | |
| CAY10509 | Prostaglandin F2α (PGF2α in prostanoid nomenclature) is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. CAY10509 is an analog of PGF2α containing a thio-fluorobenzene substituent in the lower side chain, which has an IC50 of about 30 nM for binding to the recombinant human FP receptor. Synonyms: CAY 10509; CAY-10509. Grade: ≥98%. CAS No. 1245699-47-1. Molecular formula: C23H35FO5S. Mole weight: 442.6. | |
| CAY10510 | Prostaglandin F2α (PGF2α in prostanoid nomenclature) is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. CAY10510 is an analog of PGF2α containing an acetylenic fluorobenzene substituent in the lower side chain, which has an IC50 of 0.5 nM when tested for binding to the recombinant human FP receptor. Synonyms: CAY 10510; CAY-10510. Grade: ≥98%. CAS No. 291303-34-9. Molecular formula: C24H33FO5. Mole weight: 420.5. | |
| CAY10512 | NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA, cytokine production and cell survival. CAY10512 is an analog of Resveratrol that is 100-fold more potent (IC50 = 150 nM) at inhibiting NF-κB activation by TNF-α. Unlike Resveratrol and some other trans-stilbene analogs, CAY10512 does not exhibit antioxidant activity (up to 15 μM) in either the ferric reducing/antioxidant power (FRAP) or total radical antioxidant parameter (TRAP) assays. Synonyms: (E)-2-Fluoro-4?-methoxystilbene. Grade: ≥97%. CAS No. 139141-12-1. Molecular formula: C15H13FO. Mole weight: 228.3. | |
| CAY10514 | 8(S)-HETE is a strong activator of peroxisome proliferator-activated receptors α (PPARα) and a weak activator of peroxisome proliferator-activated receptors γ (PPARγ). CAY10514 is an aromatic analog of 8(S)-HETE, which acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 μM, respectively. Synonyms: Methyl-8-hydroxy-8-(2-pentyl-oxyphenyl)-oct-5-ynoate. Grade: ≥98%. CAS No. 868526-38-9. Molecular formula: C20H28O4. Mole weight: 332.4. | |
| CAY10526 | CAY10526 is a selective mPGES-1 inhibitor that specifically inhibits PGE2 production through the modulation of mPGES1 expression without affecting COX-2. It significantly suppressed tumor growth and increased apoptosis in melanoma xenografts. Synonyms: CAY-10526; CAY 10526. Grade: >98%. CAS No. 938069-71-7. Molecular formula: C12H7BrO3S. Mole weight: 311.15. | |
| CAY10535 | TPα and TPβ are two isoforms of the human TP receptor, which is the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ with IC50 of 99 nM than TPα with IC50 of 1970 nM in the inhibition of U46619-mediated Ca2+ mobilization. Synonyms: CAY 10535; CAY-10535. Grade: ≥98%. CAS No. 945716-28-9. Molecular formula: C18H21N3O7S. Mole weight: 423.4. | |
| CAY10554 | Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively. Synonyms: BML-259; BML 259; CAY 10554; CAY-10554. Grade: ≥95%. CAS No. 267654-00-2. Molecular formula: C14H16N2OS. Mole weight: 260.4. | |
| CAY10561 | The extracellular signal-regulated kinases (ERKs) or classical MAP kinases are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 with Ki of 2 nM. It is highly selective for ERK2 and inhibits proliferation of COLO 205 cells with IC50 of 0.54 μM. Synonyms: Pyrazolylpyrrole ERK Inhibitor; CAY 10561; CAY-10561. Grade: ≥98%. CAS No. 933786-58-4. Molecular formula: C22H17Cl2FN4O2. Mole weight: 459.3. | |
| CAY10566 | Stearoyl-CoA desaturase (SCD) is an endoplasmic reticulum enzyme that catalyzes the rate-limiting step in the formation of monounsaturated fatty acids (MUFAs), specifically oleate and palmitoleate from stearoyl-CoA and palmitoyl-CoA. CAY10566 is a potent and selective SCD1 inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. It also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells. Synonyms: CAY 10566; CAY-10566. Grade: ≥98%. CAS No. 944808-88-2. Molecular formula: C18H17ClFN5O2. Mole weight: 389.8. | |
| CAY10567 | AKT1 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. CAY10567 is an AKT1 translocation inhibitor. It can prevent the translocation of AKT1 by apparently compromising the function of the PH domain. CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 μM. Synonyms: BML-257. Grade: ≥98%. CAS No. 32387-96-5. Molecular formula: C21H14N2O2. Mole weight: 326.4. | |
| CAY10570 | Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. CAY10570 is a reversible competitive inhibitor of FAAH activity exhibiting an IC50 value of 1.3 μM. It has no affinity for the human CB1 receptor and acts as a competitive inhibitor of FAAH activity without being hydrolyzed. Synonyms: CAY 10570; CAY-10570. Grade: >98%. CAS No. 875014-22-5. Molecular formula: C25H32N2OS. Mole weight: 408.6. | |
| CAY10571 | CAY10571 is a cell-permeable, reversible, and ATP-competitive sulfone analog of the p38 MAP kinase inhibitor. It is an analog of SB203580, which inhibits IL-1 production in the human monocytic cell line THP with an IC50 value of 0.20 μM and binds CSAID binding protein. Synonyms: CAY 10571; CAY-10571. Grade: ≥95%. CAS No. 152121-46-5. Molecular formula: C21H16FN3O2S. Mole weight: 393.4. | |
| CAY10573 | Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It shows stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM). Synonyms: CAY 10573; CAY-10573. Grade: ≥98%. CAS No. 853652-40-1. Molecular formula: C33H31NO5. Mole weight: 521.6. | |
| CAY10574 | Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10574, also known as Cdk9 Inhibitor II, is a potent, selective inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with Ki of 13.3 μM and IC50 values 20 μM. Synonyms: CAY 10574; CAY-10574; Cdk9 Inhibitor II. Grade: ≥95%. CAS No. 140651-18-9. Molecular formula: C9H10N6O. Mole weight: 218.2. | |
| CAY10575 | NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA, cytokine production and cell survival. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKK-α and IKK-β, can also activate NF-κB. CAY10512 is an analog of Resveratrol that is 100-fold more potent with IC50 of 150 nM at inhibiting NF-κB activation by TNF-α. It does not exhibit antioxidant activity in either the ferric reducing/antioxidant power (FRAP) or total radical antioxidant parameter (TRAP) assays. Synonyms: CAY 10575; CAY-10575. Grade: ≥95%. CAS No. 916985-21-2. Molecular formula: C22H21N3O6S2. Mole weight: 487.6. | |
| CAY10577 | Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase that has been implicated in cell cycle control, DNA repair, regulation of the circadian rhythm, and other cellular processes. Deregulation of CK2 has been linked to tumorigenesis as a potential protection mechanism for mutated cells. CAY10577 inhibits CK2 with an IC50 value of 0.8 μM. Synonyms: CAY 10577; CAY-10577. Grade: ≥95%. CAS No. 300675-28-9. Molecular formula: C10H5Cl2NO3. Mole weight: 258.1. | |
| CAY10578 | Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase that has been implicated in cell cycle control, DNA repair, regulation of the circadian rhythm, and other cellular processes. Deregulation of CK2 has been linked to tumorigenesis as a potential protection mechanism for mutated cells. CAY10578 is a potent inhibitor of CK2 with IC50 value of 0.3 μM. It is ATP competitive and displays Ki value of 0.2 μM. Synonyms: CAY 10578; CAY-10578. Grade: ≥95%. CAS No. 19231-60-8. Molecular formula: C10H3I4NO4. Mole weight: 708.8. | |
| CAY10580 | Prostaglandin E2 is a naturally occurring prostaglandin which is used as a medication. As a medication it is used in labor induction, bleeding after delivery, termination of pregnancy, and in newborn babies to keep the ductus arteriosus open. CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor with Ki of 35 nM. Synonyms: CAY 10580; CAY-10580. Grade: ≥96%. CAS No. 64054-40-6. Molecular formula: C19H35NO4. Mole weight: 341.5. | |
| CAY10581 | CAY10581 is a potent IDO inhibitor. Synonyms: CAY10581; CAY 10581; CAY-10581; 1018340-07-2; CHEMBL407954. Grade: > 98%. CAS No. 1018340-07-2. Molecular formula: C22H21NO4. Mole weight: 363.41. | |
| CAY10583 | Leukotriene B4 (LTB4) is a leukotriene involved in inflammation. It is produced from leukocytes in response to inflammatory mediators and is able to induce the adhesion and activation of leukocytes on the endothelium, allowing them to bind to and cross it into the tissue. CAY10583 is a selective and synthetic LTB4 agonist with EC50 of 20 nM. Synonyms: CAY 10583; CAY-10583. Grade: ≥98%. CAS No. 862891-27-8. Molecular formula: C25H25NO3. Mole weight: 387.5. | |
| CAY10589 | CAY10589 is a dual inhibitor of mPGES-1 with IC50 of 1.3 μM and 5-LO with IC50 of 1.0 μM. It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively. Synonyms: CAY 10589; CAY-10589. Grade: ≥98%. CAS No. 1077626-52-8. Molecular formula: C25H28ClN3O2S. Mole weight: 470. | |
| CAY10590 | Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis. There are three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2). CAY10590 is a selective and potent inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2. Synonyms: CAY 10590; CAY-10590. Grade: ≥98%. CAS No. 1101136-50-8. Molecular formula: C21H33NO3. Mole weight: 347.5. | |
| CAY10591 | Sirtuins (SIRTs) are a family of proteins that regulate cellular health. Sirtuins play a key role in regulating cellular homeostasis. SIRT1 Activator 3 is a member of the sirtuins (SIRTs), which is a distinctive class of trichostatin A-insensitive lysyl-deacetylases. CAY10591 has been shown to increase fluorescence by 233% in a SIRT1 activity assay, and to suppress TNF-α in a dose-dependent manner. It suppresses TNF-α in a dose-dependent manner. Uses: Enzyme activators. Synonyms: SIRT1 Activator 3; Sirtuin 1 Activator 3; CAY 10591; CAY-10591. Grade: ≥98%. CAS No. 839699-72-8. Molecular formula: C20H25N5O2. Mole weight: 367.5. | |
| CAY10592 | Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. CAY10592 is a full PPARδ agonist with EC50 of 30 nM in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. Synonyms: CAY 10592; CAY-10592. Grade: ≥98%. CAS No. 685139-10-0. Molecular formula: C23H17Br2ClO3S. Mole weight: 568.7. | |
| CAY10594 | Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. There are two mammalian isoforms of PLD, which are PLD1 and PLD2. CAY10594 is a potent phospholipase D2 inhibitor (PLD2), which also prevents the invasive migration of breast cancer cells. It ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. Synonyms: CAY 10594; CAY-10594. Grade: ≥98%. CAS No. 1130067-34-3. Molecular formula: C26H28N4O2. Mole weight: 428.5. | |
| CAY10595 | Chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2) is a G-protein coupled receptor that binds to the ligand prostaglandin D2 (PGD2).The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. CAY10595 is a mixture of isomers which acts as a potent CRTH2/DP2 receptor antagonist with Ki of 10 nM. Synonyms: CAY 10595; CAY-10595. Grade: ≥97%. CAS No. 916047-16-0. Molecular formula: C20H13Cl2FN2O5. Mole weight: 451.2. | |
| CAY10597 | The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. Synonyms: CAY 10597; CAY-10597. Grade: ≥98%. CAS No. 916046-55-4. Molecular formula: C20H14ClFN2O5. Mole weight: 416.8. | |
| CAY10599 | Peroxisome proliferator-activated receptor gamma (PPARγ), also known as the glitazone receptor, or NR1C3, is a type II nuclear receptor that in humans is encoded by the PPARG gene. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at PPARγ with an EC50 of 0.05 μM. It shows high selectivity for the PPARγ receptor over PPARβ (EC50 > 10 μM) or PPARα (EC50 = 3.99 μM). Synonyms: CAY 10599; CAY-10599. Grade: ≥98%. CAS No. 1143573-33-4. Molecular formula: C38H41NO5. Mole weight: 591.7. | |
| CAY10602 | Sirtuins (SIRTs) are a family of proteins that regulate cellular health. Sirtuins play a key role in regulating cellular homeostasis. CAY10602 is a cell-permeable pyrroloquinoxaline compound that acts as a reversible SIRT1 activator and enhances fat mobilization in fully differentiated 3T3L1 fibroblasts. CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. Synonyms: CAY 10602; CAY-10602. Grade: ≥95%. CAS No. 374922-43-7. Molecular formula: C22H15FN4O2S. Mole weight: 418.4. | |
| CAY10603 | CAY10603 is a potent and selective inhibitor of HDAC6 with IC50 of 2 pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively. Uses: Histone deacetylase inhibitors. Synonyms: CAY10603; CAY-10603; CAY 10603. Grade: >98%. CAS No. 1045792-66-2. Molecular formula: C22H30N4O6. Mole weight: 446.5. | |
| CAY10606 | Arachidonate 5-lipoxygenase, also known as ALOX5, 5-lipoxygenase, 5-LOX, or 5-LO, is a non-heme iron-containing enzyme that in humans is encoded by the ALOX5 gene. 5-LO initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM). It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 with IC50 of 1.6 μM. Synonyms: CAY 10606; CAY-10606. Grade: ≥98%. CAS No. 1159576-98-3. Molecular formula: C22H18ClNO3. Mole weight: 379.8. | |
| CAY10608 | The N-methyl-D-aspartate receptor (NMDA) is a glutamate receptor and ion channel protein found in nerve cells. The NMDA receptor is one of three types of ionotropic glutamate receptors. The other receptors are the AMPA and kainate receptors. NMDA is Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors with IC50 of 50 nM. Synonyms: CAY 10608; CAY-10608. Grade: ≥98%. CAS No. 457897-92-6. Molecular formula: C18H22Cl2N2O4S. Mole weight: 433.4. | |
| CAY10614 | Lipid A is a lipid component of an endotoxin held responsible for the toxicity of gram-negative bacteria. It is the innermost of the three regions of the lipopolysaccharide (LPS), also called endotoxin molecule, and its hydrophobic nature allows it to anchor the LPS to the outer membrane. A activates toll-like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC50 value of 1.68 μM. It does not significantly affect HEK cell viability. Synonyms: CAY 10614; CAY-10614. Grade: ≥98%. CAS No. 1202208-36-3. Molecular formula: C42H78INO2. Mole weight: 756. | |
| CAY10621 | Sphingosine kinase (SphK) is a conserved lipid kinase that catalyzes formation sphingosine-1-phosphate (S1P) from the precursor sphingolipid sphingosine. The two known kinases, sphingosine kinase 1 (SphK1) and sphingosine kinase 2 (SphK2), have different developmental and tissue expression patterns, suggesting that they have distinct physiological functions. CAY10621 is an inhibitor of SPHK1 with IC50 of 3.3 μM. It is selective for SphK1 over Sph2 at 10 μM and PKC at concentrations less than 100 μM. CAY10621 inhibits SphK1 activity by 70% in U937 cells at 5 μM. Synonyms: SKI 5C; SPHK1 Inhibitor 5C; CAY 10621; CAY-10621. Grade: ≥98%. CAS No. 120005-55-2. Molecular formula: C26H45NO4. Mole weight: 435.6. | |
| CAY10622 | Rho-associated protein kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton. Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions. CAY10622 is a potent, ureidobenzamide inhibitor of ROCK-I and ROCK-II kinases with IC50 values of 6 and 4 nM, respectively. Synonyms: CAY 10622; CAY-10622. Grade: ≥98%. CAS No. 1038549-25-5. Molecular formula: C25H25N5O3. Mole weight: 443.5. | |
| CAY10626 | Phosphatidylinositol 3-kinases (PI3K) are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. PI3K catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. CAY10626 demonstrates IC50 values of <3 and 13 nM for MDA361 (breast) and PC3 (prostate) cancer cell lines, respectively. Synonyms: CAY 10626; CAY-10626. Grade: ≥98%. CAS No. 1202884-94-3. Molecular formula: C31H35F3N8O3. Mole weight: 624.7. | |
| CAY10638 | Peroxisome proliferator-activated receptor gamma (PPARγ), also known as the glitazone receptor, or NR1C3, is a type II nuclear receptor that in humans is encoded by the PPARG gene. Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity. CAY10638 is a TZD derivative that inhibits 15-PGDH activity with IC50 of 31 nM. Synonyms: CAY 10638; CAY-10638. Grade: ≥98%. CAS No. 1221413-57-5. Molecular formula: C16H13NO3S2. Mole weight: 331.4. | |
| CAY10640 | Soluble epoxide hydrolase (sEH) is a bifunctional enzyme that in humans is encoded by the EPHX2 gene. sEH is a member of the epoxide hydrolase family. CAY10640 is a 1-aryl-3-(1-acylpiperidin-4-yl)urea analog that inhibits recombinant human and mouse sEH with IC50 values both equal to 0.4 nM. Synonyms: sEHi; Soluble Epoxide Hydrolase Inhibitor; CAY 10640; CAY-10640. Grade: ≥98%. CAS No. 1208549-68-1. Molecular formula: C17H20F3N3O3. Mole weight: 371.4. | |
| CAY10649 | Arachidonate 5-lipoxygenase, also known as ALOX5, 5-lipoxygenase, 5-LOX, or 5-LO, is a non-heme iron-containing enzyme that in humans is encoded by the ALOX5 gene. 5-LO initiates the synthesis of (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10649 is a thiazolinone compound that demonstrates direct inhibition of 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) with IC50 of 0.28 μM. Synonyms: CAY 10649; CAY-10649. Grade: ≥98%. CAS No. 1272519-89-7. Molecular formula: C17H12ClNO2S. Mole weight: 329.8. | |
| CAY10650 | Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process. CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor. It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis. Synonyms: CAY 10650; CAY-10650. Grade: >98%. CAS No. 1233706-88-1. Molecular formula: C28H25NO6. Mole weight: 471.5. | |
| CAY10669 | P300/CBP-associated factor (PCAF), also known as K(lysine) acetyltransferase 2B (KAT2B), is a co-activator of p53-target genes and moreover it regulates p53 activity by acetylating K320, which promotes p53-dependent p21 transcription and cell cycle arrest during DNA damage. CAY10669 is an inhibitor of the histone acetyltransferase PCAF, which displays 2-fold improvement in inhibitory potency over anacardic acid. Synonyms: CAY 10669; CAY-10669. Grade: ≥98%. CAS No. 1243583-88-1. Molecular formula: C20H22O4. Mole weight: 326.4. | |
| CAY10677 | Isoprenylcysteine Carboxyl Methyltransferase (ICMT) is a protein coding gene. Diseases associated with ICMT include Hallermann-Streiff syndrome and Legionnaire disease. CAY10677 is an analog of the ICMT inhibitor cysmethynil that was developed for improved solubility and cell permeability. It inhibits ICMT with an IC50 value of 0.86 μM and demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells and human prostate cancer PC3 cells. Synonyms: Icmt Inhibitor 15; CAY 10677; CAY-10677. Grade: ≥98%. CAS No. 1443253-20-0. Molecular formula: C25H37N5. Mole weight: 407.6. | |
| CAY10678 | Microsomal prostaglandin E synthase-1 (mPGES-1) or Prostaglandin E synthase is an enzyme that in humans is encoded by the PTGES gene. The protein encoded by this gene is a glutathione-dependent prostaglandin E synthase. The IC50s of mPGES-1 inhibitor are 900 nM for human and 90 nM for rat. CAY10678 is a selective microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor. Synonyms: mPGES-1 Inhibitor III; CAY 10678; CAY-10678. Grade: ≥98%. CAS No. 1268709-57-4. Molecular formula: C23H34N4O. Mole weight: 382.5. | |
| CAY10680 | The monoamine oxidases A and B are the products of two abutting X-linked genes, and play an important role in the metabolism of biogenic amines in the central nervous system. Inhibition of MAO-B is considered as a strategy to treat Parkinson's disease. CAY10680 is a benzothiazinone compound that selectively inhibits MAO-B with IC50 = 34.9 nM in human. The blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. It can selectively inhibits with Ki of 39.5 nM in human. Synonyms: CAY 10680; CAY-10680. Grade: ≥98%. CAS No. 1439488-21-7. Molecular formula: C18H16N2O2S. Mole weight: 324.4. | |
| CAY10681 | NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA, cytokine production and cell survival. CAY10681 is an orally active, small molecule that inhibits p53-MDM2 interaction and NF-κB pathway thus inhibiting tumor growth. It also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. Synonyms: CAY 10681; CAY-10681. Grade: ≥98%. CAS No. 1542066-69-2. Molecular formula: C30H26BrN5O. Mole weight: 552.5. | |
| CAY10682 | The MDM2 protein is a negative regulator of p53. After binding to p53, it inhibits its transcriptional activity, favours its nuclear export and stimulates its degradation. The MDM2-TP53 pathway is a tumor-suppressor pathway that is often disrupted in cancer. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 with Ki of 83 nM. It also blocks the growth of cancer cells with IC50 of 2-6 μM in vitro and inhibits the growth of A549 cell xenografts in mice. Synonyms: CAY 10682; CAY-10682. Grade: ≥98%. CAS No. 1542066-74-9. Molecular formula: C30H25BrFN5O. Mole weight: 570.5. | |
| CAY10683 | CAY10683 is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, > 3600-fold selectivity over other HDACs. Uses: Histone deacetylase inhibitors. Synonyms: CAY-10683; CAY 10683; Santacruzamate A. Grade: >98%. CAS No. 1477949-42-0. Molecular formula: C15H22N2O3. Mole weight: 278.35. | |
| CAY10684 | Prostaglandin E2 receptor 4 (EP4) is a prostaglandin receptor for prostaglandin E2 (PGE2) encoded by the PTGER4 gene in humans. EP4 is a G protein-coupled receptor, which plays important roles in bone formation and resorption. CAY10684 is an EP4 receptor agonist. It displays more than 1,000-fold selectivity for EP4 over other EP receptors. Synonyms: CAY 10684; CAY-10684; 7-((2R)-2-((E)-3-(4'-Chloro-2'-methyl-[1,1'-biphenyl]-3-yl)-3-hydroxyprop-1-en-1-yl)-5-oxopyrrolidin-1-yl)heptanoic acid. Grade: ≥98%. CAS No. 493035-81-7. Molecular formula: C27H32ClNO4. Mole weight: 470. | |
| CAY10685 | CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. CAY10685 is a cell-active analog of the lysine acetyltransferase inhibitor CPTH2 that contains an alkyne moiety. It can inhibit N-acetyltransferase, which shows potential applicaiton in studying the changes in nuclear architecture associated with cancer and certain laminopathies. Synonyms: CAY 10685; CAY-10685. Grade: ≥98%. CAS No. 1613116-16-7. Molecular formula: C17H16ClN3S. Mole weight: 329.8. | |
| CAY10698 | Platelet-type 12-lipoxygenase (12-LO) catalyzes the formation of 12-HpETE from arachidonic acid, which has been found to be expressed in various tumor cells. CAY10698 is an inhibitor of 12-LO with an IC50 value of 5.1 uM. It shows potenital applicaiton in biological characterization for development of potential 12-LO inhibitors. Synonyms: CAY 10698; CAY-10698. Grade: ≥98%. CAS No. 684236-01-9. Molecular formula: C17H17N3O4S2. Mole weight: 391.5. | |
| CAY10700 | Microsomal prostaglandin E synthase-1 (mPGES-1) or Prostaglandin E synthase is an enzyme that in humans is encoded by the PTGES gene. The protein encoded by this gene is a glutathione-dependent prostaglandin E synthase. CAY10700 is a novel selective and orally bioavailable inhibitor of mPGES-1 with IC50 of 0.24 μM for human whole blood assay. Uses: Enzyme inhibitors. Synonyms: mPGES-1 Inhibitor-1; CAY 10700; CAY-10700. Grade: ≥98%. CAS No. 1381846-21-4. Molecular formula: C16H19ClN4O2. Mole weight: 334.8. | |
| CAY10711 | CAY10711 is a substituted diamine that produces rapid bactericidal activity against both Gram-positive and Gram-negative bacteria. It can reduce biofilm formation and promotes biofilm dispersal in P. aeruginosa. CAY10711 displays MIC99 values of 2.9, 11.5, 2.9, and 2.9 μM against S. aureus RN4220, P. aeruginosa PAO1, E. coli ANS1, and MRSA 10082B, respectively. Synonyms: CAY 10711; CAY-10711. Grade: ≥95%. CAS No. 1666171-29-4. Molecular formula: C41H54N6S2. Mole weight: 695. | |
| CAY10717 | CAY10717 is a multi-targeted kinase inhibitor that exhibits greater than 40% inhibition of 34 of 104 kinases in an enzymatic assay at 100 nM. CAY10717 is highly cytotoxic against a cancer cell panel that includes chemotherapy-sensitive and -resistant cell lines (EC50s = 0.4-158 nM). It also inhibits the growth of human umbilical vein endothelial cells (HUVECs) with EC50 of 34 nM. Synonyms: CAY 10717; CAY-10717. Grade: ≥95%. CAS No. 1240322-54-6. Molecular formula: C29H25F3N6O3. Mole weight: 562.5. | |
| CAY10719 | ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects many tissues against xenobiotic molecules. CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 with IC50 of 0.23 μM. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and inhibit ATPase activity. Synonyms: CAY 10719; CAY-10719. Grade: ≥98%. CAS No. 1942919-63-2. Molecular formula: C25H20Cl2N2O2. Mole weight: 451.3. | |
| CAY10721 | Sirtuins (SIRTs) are a family of proteins that regulate cellular health. Sirtuins play a key role in regulating cellular homeostasis. SIRT1 Activator 3 is a member of the sirtuins (SIRTs), which is a distinctive class of trichostatin A-insensitive lysyl-deacetylases. CAY10721 is an inhibitor of SIRT3. It is a class III HDAC (39% SIRT3 inhibition at 200 μM). Synonyms: CAY 10721; CAY-10721. Grade: ≥98%. CAS No. 848688-62-0. Molecular formula: C18H13N3O3S. Mole weight: 351.4. | |
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