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CAY10722
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. CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). Synonyms: CAY 10722; CAY-10722. Grade: ≥98%. CAS No. 388086-13-3. Molecular formula: C21H14Cl2N2O2. Mole weight: 397.3.
CAY10729 trifluoroacetate salt
Peptidyl Arginine Deiminases (PADs) perform post-translational deiminations of proteins. PADs are calcium-dependent enzymes that catalyze the conversion of L-arginine residues to L-citrulline. CAY10729 is a tetrazole derivative of the PAD inhibitor Cl-amidine that selectively inhibits PAD1 over PAD2, PAD3, and PAD4 (kinact/KI = 162,200, 60,000, 17,500, and 25,400 M-1min-1 for PAD1-4, respectively). Synonyms: CAY 10729; CAY-10729. Grade: ≥70%. Molecular formula: C19H26ClN7O3·xCF3COOH. Mole weight: 435.91.
CAY10734
Sphingosine-1-phosphate receptor (S1P) modulators are a class of drugs used as immunomodulators, most notably in cases of multiple sclerosis. CAY10734 is an agonist of sphingosine-1-phosphate receptor 1 (S1P1) with IC50=0.6 nM). It selectively binds S1P1 over S1P2, S1P3, and S1P4 receptors (IC50s = >10,000, 12,000, and 70 nM, respectively) but does also bind S1P5 receptors (IC50 = 1 nM) in radioligand binding assays. Synonyms: CAY 10734; CAY-10734. Grade: ≥98%. CAS No. 635701-59-6. Molecular formula: C23H25N3O3. Mole weight: 391.5.
CAY10739
Sphingosine-1-phosphate receptor (S1P) modulators are a class of drugs used as immunomodulators, most notably in cases of multiple sclerosis. CAY10739 is a soft-drug agonist of the sphingosine-1-phosphate receptor 1 (S1P1) with IC50=25.12 nM in a β-arrestin recruitment assay, which was designed to prevent systemic effects following topical application. It is selective for S1P1 over S1P2, S1P3, and S1P4 (IC50s = 1,000, >10,000, >10,000 nM, respectively). Synonyms: CAY 10739; CAY-10739. Grade: ≥98%. Molecular formula: C23H24N2O3S. Mole weight: 408.51.
CAY10781
CAY10781, an inhibitor of the protein-protein interaction between neuropilin-1 (NRP-1) and VEGF-A, inhibits the interaction by 43% at a concentration of 12.5 μM. At the same concentration, CAY10781 also inhibits VEGF-A-induced VEGFR2 phosphorylation in catecholamine-A-differentiated (CAD) cells. Synonyms: 2-(6-Oxo-2-(pyridin-3-yl)-1,6-dihydropyrimidin-5-yl)acetic acid; [6-oxo-2-(pyridin-3-yl)-1,6-dihydropyrimidin-5-yl]acetic acid; 5-Pyrimidineacetic acid, 3,4-dihydro-4-oxo-2-(3-pyridinyl)-; 3,4-Dihydro-4-oxo-2-(3-pyridinyl)-5-pyrimidineacetic acid. Grade: ≥95%. CAS No. 1210360-87-4. Molecular formula: C11H9N3O3. Mole weight: 231.21.
CB096
CB096 selectively inhibited repeat associated non-ATG (RAN) translation and decreased the production of poly(GP) DPRs without affecting r(G4C2)66 mRNA levels in an HEK293T cellular model of c9ALS/FTD, alleviated dysfunctional nucleocytoplasmic transport, and selectively reduced the abundance of r(G4C2)66-induced stress granules. Synonyms: 2-Methoxy-4-(5-nitro-1H-benzo[d]imidazol-2-yl)phenol. Grade: 99%. CAS No. 108883-90-5. Molecular formula: C14H11N3O4. Mole weight: 285.25.
CB10-277
CB10-277 is a synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alkylates DNA, resulting in inhibition of DNA replication and repair; in addition, this agent may act as a purine analogue, resulting in inhibition of DNA synthesis, and may interact with protein sulfhydryl groups. Uses: Antineoplastic agents. Synonyms: CB10-277; CB10 277; CB10277; 1-p-carboxy-3,3-dimethylphenyltriazine. CAS No. 7203-91-0. Molecular formula: C9H11N3O2. Mole weight: 193.21.
CB1151
CB1151, a 20-epi analogue of 1,25-dihydroxyvitamin D3, has potent antitumor effects and inhibits MCF-7 cell growth with an IC50 of 0.82 nM. Synonyms: 1,3-Cyclohexanediol, 5-[(2E)-[(1S,3aS,7aS)-1-[(1R)-1-[(3-ethyl-3-hydroxypentyl)oxy]ethyl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-, (1R,3S,5Z)-; (1S,3R,5Z,7E,9ξ)-20-[(3-Ethyl-3-hydroxypentyl)oxy]-9,10-secopregna-5,7,10-triene-1,3-diol. Grade: ≥95%. CAS No. 182369-28-4. Molecular formula: C28H46O4. Mole weight: 446.66.
CB181963
CB181963 shows excellent activity against MRSA strains resistant to other cephalosporins in both planktonic and biofilm cultures. It is a potent antistaphylococcal agent with better activity against MRSA. It may play a role in the treatment of staphylococcal infections, including those caused by MRSA and in the prophylaxis of biofilm-associated MSSA and MRSA infections. Uses: Cb181963 may play a role in the treatment of staphylococcal infections, including those caused by mrsa and in the prophylaxis of biofilm-associated mssa and mrsa infections. Synonyms: CB 181963; CB-181963; 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2Z)-(5-amino-1,2,4-thiadiazol-3-yl)((fluoromethoxy)imino)acetyl)amino)-3-((E)-((imino-1-piperazinylmethyl)methylhydrazono)methyl)-8-oxo-, (6R,7R)-. Grade: 98%. CAS No. 635292-67-0. Molecular formula: C19H24FN11O5S2. Mole weight: 569.59.
CB 1837
CB 1837 was the parent member of a series of nitrophenyl aziridines evaluated for antitumour activity by Khan and Ross. Synonyms: 1-(2,4-dinitrophenyl)aziridine; CB 1837; CB1837; CB-1837; AI3-51871; NSC 3375. Grade: 95%. CAS No. 27141-65-7. Molecular formula: C8H7N3O4. Mole weight: 209.159.
CB1 antagonist 1
CB1 antagonist 1 is a CB1 receptor antagonist, used for the study of metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, gastrointestinal diseases and cardiovascular diseases. Synonyms: Benzonitrile, 3-chloro-4-[2-(4-chlorophenyl)?-4-[1-(4-cyanophenyl)?ethyl]?-1-piperazinyl]?-; 3-Chloro-4-{2-(4-chlorophenyl)-4-[1-(4-cyanophenyl)ethyl]-1-piperazinyl}benzonitrile. Grade: ≥97%. CAS No. 890037-68-0. Molecular formula: C26H22Cl2N4. Mole weight: 461.39.
CB1-IN-1
CB1-IN-1 is an antagonist of cannabinoid receptor type 1 (CB1R) located in the peripheral nervous system, which may be significant for pain modulation. Synonyms: DBPR211; DBPR 211; DBPR-211; CB1-IN-1; CB1-IN 1; CB1-IN1; 1-(2,4-dichlorophenyl)-N-piperidin-1-yl-4-[(pyrrolidin-1-ylsulfonylamino)methyl]-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]thiophen-2-yl]pyrazole-3-carboxamideCB1-IN-1SCHEMBL14816497CS-5144; HY-12790; CS 5144; HY 12790; CS5144; HY12790N-Piperidino-1-(2,4-dichlorophenyl)-4-(pyrrolizinosu. CAS No. 1429239-98-4. Molecular formula: C33H31Cl2F3N6O3S2. Mole weight: 751.67.
CB1 inverse agonist 1
CB1 inverse agonist 1 is a highly potent, orally active and specific CB1 receptor inverse agonist with IC50s of 7.5 and 4100 nM for CB1 and CB2 receptors, respectively. It has anorexigenic effects. Synonyms: Acetamide, N-[3-acetyl-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-1,2-dihydro-1-methyl-2-oxo-1,8-naphthyridin-4-yl]-; Naphthyridinone; N-[3-Acetyl-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-1-methyl-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]acetamide; VUN15005; VUN-15005; VUN 15005; MRL-CB1-NC. Grade: 98%. CAS No. 852315-00-5. Molecular formula: C25H18Cl3N3O3. Mole weight: 514.79.
CB-25
Δ9-Tetrahydrocannabinol (THC) is the primary psychoactive constituent of cannabis and an active cannabinoid pharmacotherapy component. Anandamide (AEA), also known as N-arachidonoylethanolamine, is an endogenous lipid with cannabinergic activity. CB-25 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 5.2 and 13 nM, respectively. Synonyms: CB25; CB 25. Grade: ≥98%. CAS No. 869376-63-6. Molecular formula: C25H41NO3. Mole weight: 403.6.
CB2 modulator 1
CB2 modulator 1 is a potent CB2 modulator, which has the potential for immunedisorders, inflammation, osteoporosis and renal ischemia. Synonyms: 2-Anilino-N-(tetrahydro-2H-pyran-4-ylmethyl)-4-(trifluoromethyl)-5-pyrimidinecarboxamide; 5-Pyrimidinecarboxamide, 2-(phenylamino)-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-. Grade: 98%. CAS No. 666261-80-9. Molecular formula: C18H19F3N4O2. Mole weight: 380.36.
CB2R-IN-1
CB2R-IN-1 is a potent inverse agonist of cannabinoid CB2 receptor with a Ki of 0.9 nM. Synonyms: 1,1,1-Trifluoro-N-[[4-propyl-1-[[1-(2-pyridinylsulfonyl)-1H-indol-2-yl]sulfonyl]-4-piperidinyl]methyl]methanesulfonamide; Methanesulfonamide, 1,1,1-trifluoro-N-[[4-propyl-1-[[1-(2-pyridinylsulfonyl)-1H-indol-2-yl]sulfonyl]-4-piperidinyl]methyl]-. Grade: ≥97%. CAS No. 1257555-79-5. Molecular formula: C23H27F3N4O6S3. Mole weight: 608.67.
CB 300919
CB 300919 is a water-soluble analogue of CB30865; has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft. Synonyms: CB-300919; CB300919; CB 300919; UNII-55I8ETE76Y. Grade: >98%. CAS No. 289715-28-2. Molecular formula: C32H34ClN7O2. Mole weight: 584.11.
CB30865
CB30865 is a highly potent cytotoxic agent. The compound inhibits isolated mammalian thymidylate synthase (TS), but this inhibition is insufficient to account for its cellular toxicity. Thymidylate synthase (TS) is a critical enzyme in the de novo synthesis of thymidylate (dTTP) and has long been recognized as a target for chemotherapeutic intervention. Synonyms: CB-30865; CB 30865; CB30865; ZM 242421; ZM242421; ZM-242421. Grade: >98%. CAS No. 206275-15-2. Molecular formula: C26H22BrN5O2. Mole weight: 516.39.
CB30900
CB30900 has been found to be a thymidylate synthase inhibitor that could have some extent of activity in models with low or defective folylpolyglutamate synthetase. Synonyms: CB 30900; CB30900; CB-30900; N-(N-(4-(N-((3,4-Dihydro-2,7-dimethyl-4-oxo-6-quinazolinyl)methyl)-N-prop-2-ynylamino)-2-fluorobenzoyl)-L-gamma-glutamyl)-D-glutamic acid. Grade: 98%. CAS No. 145788-82-5. Molecular formula: C31H32FN5O9. Mole weight: 637.61.
CB 3703
CB 3703 is an inhibitor of hydrofolate reductase. Uses: An inhibitor of hydrofolate reductase. Synonyms: CB 3703; CB3703; CB-3703; NSC 289522. N-(p-(((2,4-Diamino-5-methyl-6-quinazolinyl)methyl)amino)benzoyl)-L-glutamic acid; L-Glutamic acid, N-(4-(((2,4-diamino-5-methyl-6-quinazolinyl)methyl)amino)benzoyl)-. Grade: ≥95%. CAS No. 32093-09-7. Molecular formula: C22H24N6O5. Mole weight: 452.18.
CB 3731
CB 3731 can be used in fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase. Synonyms: CB 3731; CB-3731; CB3731. N-(4-((N-(2-Amino-4-hydroxy-6-quinazolinyl)methyl)-N-(fluoroethyl)amino)benzoyl)glutamic acid. Grade: 98%. CAS No. 80015-07-2. Molecular formula: C23H24FN5O6. Mole weight: 458.47.
CB-3988
CB 3988 is a bio-active chemical compound. Synonyms: CB 3988; CB-3988; CB3988. (2S)-2-[2-Trifluoromethyl-4-[N-[(3,4-dihydro-2-methyl-4-oxoquinazolin)-6-ylmethyl]-N-(2-propynyl)amino]benzoylamino]glutaric acid; N-[2-Trifluoromethyl-4-[2-propynyl[(3,4-dihydro-4-oxo-2-methylquinazolin)-6-ylmethyl]amino]benzoyl]-L-glutamic acid; (2S)-2-[[4-[(2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-2-(trifluoromethyl)benzoyl]amino]pentanedioic acid. Grade: >98%. CAS No. 112888-26-3. Molecular formula: C26H23F3N4O6. Mole weight: 544.48.
CB-403
CB-403, a cinnamaldehyde derivative, which has antitumor effect through the arrest of cell cycle progression in the G2/M phase. Uses: Antitumor effect through the arrest of cell cycle progression in the g2/m phase. Synonyms: CB-403; CB403; CB 403; UNII-4V9Q0C88UK. 2-Propenal, 3-[2-[(2-methylphenyl)?methoxy]?phenyl]?-, (2E)?-. Grade: ≥96%. CAS No. 302356-18-9. Molecular formula: C17H16O2. Mole weight: 252.11.
CB5083
CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer. Synonyms: CB5083; CB-5083; CB 5083. Grade: >98%. CAS No. 1542705-92-9. Molecular formula: C24H23N5O2. Mole weight: 413.4.
CB-52
Δ9-Tetrahydrocannabinol (THC) is the primary psychoactive constituent of cannabis and an active cannabinoid pharmacotherapy component. Anandamide (AEA), also known as N-arachidonoylethanolamine, is an endogenous lipid with cannabinergic activity. CB-52 is a stable analog of Δ9-tetrahydrocannabinol (THC) and anandamide (AEA). It exhibits high affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 210 and 30 nM, respectively. Synonyms: CB52; CB 52. Grade: ≥98%. CAS No. 869376-90-9. Molecular formula: C26H43NO3. Mole weight: 417.6.
CB 65
CB 65 is a high affinity and selective CB2 receptor agonist with Ki of 3.3 nM for CB2 receptor and Ki of > 1000 nM for CB1 receptor. Uses: Cannabinoid receptor agonists. Synonyms: N-Cyclohexyl-7-chloro-1-[2-(4-morpholinyl)ethyl]quinolin-4(1H)-one-3-carboxamide. Grade: ≥99%. CAS No. 913534-05-1. Molecular formula: C22H28ClN3O3. Mole weight: 417.93.
CB-6644
CB-6644 is a novel allosteric selective inhibitor of the ruvbl1/2 complex with anti-cancer activity. It blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM. Synonyms: CB 6644; CB6644. CAS No. 2316817-88-4. Molecular formula: C29H34ClFN4O5. Mole weight: 573.06.
CB7646
CB7646 is a stable analogue of trimelamol (TM). It is used as an anti-tumour agent. Uses: Cb7646 is used as an anti-tumour agent. Synonyms: CB-7646; CB 7646; CB7646; UNII-LYO93N5MEB. Methanol, ((6-(methylamino)-1,3,5-triazine-2,4-diyl)bis(methylimino))bis-; [[4-[Hydroxymethyl(methyl)amino]-6-(methylamino)-1,3,5-triazin-2-yl]-methylamino]methanol. Grade: >98 %. CAS No. 104880-54-8. Molecular formula: C8H16N6O2. Mole weight: 228.25.
CB-7921220
CB-7921220 is an adenylate cyclase inhibitor which is selective, reducing adenylyl cyclase type I and VI activity by 60% while having no effect on types II and V in Sf9 membranes stimulated by forskolin at a concentration of 100 μM. CB-7921220 has a binding conformation similar to ATP and P-site inhibitors, which may explain its lack of selectivity between AC1 and AC6. Synonyms: CB7921220; CB 7921220; CB-7921220; 6-[(E)-2-(4-aminophenyl)ethenyl]pyridine-2-carboxylic acid. CAS No. 115453-99-1. Molecular formula: C14H12N2O2. Mole weight: 240.26.
CB-839
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. Upon oral administration, CB-839 selectively and irreversibly inhibits glutaminase, a mitochondrial enzyme that is essential for the conversion of the amino acid glutamine into glutamate. By blocking glutamine utilization, proliferation in rapidly growing cells is impaired. Glutamine-dependent tumors rely on the conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). ( ). Synonyms: CB-839; CB839; CB 839. Grade: 98%. CAS No. 1439399-58-2. Molecular formula: C26H24F3N7O3S. Mole weight: 571.57.
CB-86
Cannabinoid receptors (CB) are of a class of cell membrane receptors in the G protein-coupled receptor superfamily. CB-86 is a resorcinol-anandamide hybrid compound that acts as a partial agonist for the CB1 receptor with Ki of 5.6 nM and a neutral antagonist for CB2 receptor with Ki of 7.9 nM. CB-86 exhibits antinociceptive effects in mice treated with formalin. Synonyms: CB86; CB 86. Grade: ≥98%. CAS No. 1150586-64-3. Molecular formula: C26H43NO3. Mole weight: 417.6.
CB 966
CB 966 is a novel analogues of 1,25-dihydroxyvitamin D3 and it was found to significantly delay the rejection of allogeneic skin grafts in CBA (H-2k) recipient mice. Synonyms: CB 966; CB966; CB-966. (1R-(1alpha(R*),3abeta,4E(1R*,3S*,5Z),7aalpha))-5-((1-(6-ethyl-6-hydroxy-1-methyloctyl)octahydro-7a-methyl-4H-inden-4-ylidene)ethylidene)-4-methylene-1,3-Cyclohexanediol. Grade: 98%. CAS No. 128312-71-0. Molecular formula: C30H50O3. Mole weight: 458.72.
CBA
Transient Receptor Potential Cation Channel Subfamily M Member 4 (TRPM 4) is a Protein Coding gene. Diseases associated with TRPM4 include Progressive Familial Heart Block, Type Ib and Erythrokeratodermia Variabilis Et Progressiva. TRPM4-IN-5 is a potent and selective inhibitor of the cation channel TRPM4 blocker with IC 50 of 1.5 μM. Synonyms: 4-Chloro-2-[[2-(2-chlorophenoxy)acetyl]amino]benzoic acid; TRPM4-IN-5; TRPM4IN-5; TRPM4-IN5; TRPM4 IN-5. Grade: ≥98%. CAS No. 351424-20-9. Molecular formula: C15H11Cl2NO4. Mole weight: 340.16.
CBB1003
CBB1003, a piperazine derivative, has been found to be a histone demethylase LSD1 inhibitor that could restrain the proliferation and colony formation of CRC cell in mice. IC50: 10.54 uM. Uses: Cbb1003 has been found to be a histone demethylase lsd1 inhibitor that could restrain the proliferation and colony formation of crc cell in mice. Synonyms: CBB1003; SCHEMBL16273292; CS-3476. Grade: 98%. CAS No. 1379573-88-2. Molecular formula: C25H31N9O4. Mole weight: 521.57.
CBB1003 hydrochloride
CBB1003 hydrochloride is an inhibitor of histone demethylase LSD1 with an IC50 of 10.54 μM. Synonyms: 4-(3-{[4-(4-Carbamimidoylbenzoyl)-1-piperazinyl]carbonyl}-5-nitrobenzyl)-1-piperazinecarboximidamide pentahydrochloride; 1-Piperazinecarboximidamide, 4-[[3-[[4-[4-(aminoiminomethyl)benzoyl]-1-piperazinyl]carbonyl]-5-nitrophenyl]methyl]-, hydrochloride (1:5). Molecular formula: C25H36Cl5N9O4. Mole weight: 703.88.
CBB1007
CBB1007, an amidino-guanidinium derivative, has been found to have biological activity in anticancer-study by acting as a LSD1 inhibitor. IC50: 5.27 uM. Uses: Cbb1007 has been found to have biological activity in anticancer-study by acting as a lsd1 inhibitor. Synonyms: CBB1007; SCHEMBL16273312; CS-1737. Grade: 98%. CAS No. 1379573-92-8. Molecular formula: C27H34N8O4. Mole weight: 534.61.
CBB1007 hydrochloride
CBB1007 hydrochloride, a cell-permeable amidino-guanidinium compound, is a potent, reversible and substrate competitive LSD1 selective inhibitor with an IC50 of 5.27 μM for hLSD1. Synonyms: Methyl 3-{[4-(4-carbamimidoylbenzoyl)-1-piperazinyl]carbonyl}-5-[(4-carbamimidoyl-1-piperazinyl)methyl]benzoate pentahydrochloride; Benzoic acid, 3-[[4-[4-(aminoiminomethyl)benzoyl]-1-piperazinyl]carbonyl]-5-[[4-(aminoiminomethyl)-1-piperazinyl]methyl]-, methyl ester, hydrochloride (1:5). Grade: ≥98%. Molecular formula: C27H39Cl5N8O4. Mole weight: 716.91.
CBB1007 trihydrochloride
CBB1007 trihydrochloride, a cell-permeable amidino-guanidinium compound, is a potent, reversible and substrate competitive LSD1 selective inhibitor with an IC50 of 5.27 μM for hLSD1. Synonyms: Methyl 3-{[4-(4-carbamimidoylbenzoyl)-1-piperazinyl]carbonyl}-5-[(4-carbamimidoyl-1-piperazinyl)methyl]benzoate trihydrochloride; Benzoic acid, 3-[[4-[4-(aminoiminomethyl)benzoyl]-1-piperazinyl]carbonyl]-5-[[4-(aminoiminomethyl)-1-piperazinyl]methyl]-, methyl ester, hydrochloride (1:3). Grade: ≥96%. Molecular formula: C27H37Cl3N8O4. Mole weight: 643.99.
CBFβ Inhibitor
Core binding factors (CBFs) are heterodimeric transcription factors containing a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ. CBFβ Inhibitor cellular studies indicate a good correlation between the inhibitor's antiproliferative activity and the Runx1 expression level in the target cells. Synonyms: Core Binding Factor-β Inhibitor; 2-Thiazolamine, 5-ethyl-4-(4-methoxyphenyl)-; 5-Ethyl-4-(4-methoxyphenyl)-2-thiazolamine; Sc 221405; 5-Ethyl-4-(4-methoxy-phenyl)-thiazol-2-ylamine. Grade: ≥98%. CAS No. 493028-20-9. Molecular formula: C12H14N2OS. Mole weight: 234.32.
CBHA
Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. CBHA is a cell-permeable second generation hybrid polar agent that acts as a HDAC inhibitor. It exhibits ID50 values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively. CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture. Uses: Histone deacetylase inhibitors. Synonyms: Histone Deacetylase Inhibitor II; m-Carboxycinnamic acid bis-hydroxamide. Grade: ≥98%. CAS No. 174664-65-4. Molecular formula: C10H10N2O4. Mole weight: 222.2.
CBiPES hydrochloride
CBiPES hydrochloride is a selective positive allosteric modulator of the mGlu2 receptor (IC50 = 98.2 nM). Synonyms: N-(4'-Cyano-[1,1'-biphenyl]-3-yl-N-(3-pyridinylmethyl)-ethanesulfonamide hydrochloride. Grade: ≥99% by HPLC. CAS No. 856702-40-4. Molecular formula: C21H19N3O2S.HCl. Mole weight: 413.92.
CBL0137
CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 μM and inhibits NF-κB with an EC50 of 0.47 μM. It also inhibits histone chaperone FACT (facilitates chromatin transcription) and MYC signal. Synonyms: CBL0137; CBL-0137; CBL 0137; CBLC137; CBLC-137; CBLC 137; Curaxin 137; 1,1'-(9-(2-(Isopropylamino)ethyl)-9H-carbazole-3,6-diyl)diethanone; 1-[6-acetyl-9-[2-(propan-2-ylamino)ethyl]carbazol-3-yl]ethanone. CAS No. 1197996-80-7. Molecular formula: C21H24N2O2. Mole weight: 336.435.
CBL0137 hydrochloride
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. CBL0137 activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death. Synonyms: CBLC137; CBL-0137; Curaxin 137. Grade: ≥98%. CAS No. 1197397-89-9. Molecular formula: C21H24N2O2·HCl. Mole weight: 372.9.
Cbl-b-IN-3
Cbl-b-IN-3 inhibits proto-oncogene-B (CPL-B). CBL-B is an E3 ubiquitin ligase that ubiquitinates proteins downstream of immune receptors to downregulate positive signaling cascades. Synonyms: 2-{3-[(1S,3R)-3-methyl-1-(4-methyl-4H-1,2,4-triazol-3-yl)cyclobutyl]phenyl}-6-{[(3S)-3-methylpiperidin-1-yl]methyl}-4-(trifluoromethyl)-2,3-dihydro-1H-isoindol-1-one. Grade: >98.0%. CAS No. 2573775-59-2. Molecular formula: C30H34F3N5O. Mole weight: 537.63.
CBP501
CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle. Check for active clinical trials or closed clinical trials using this agent. Synonyms: CBP-501; CBP 501; H-D-Bpa-D-Ser-D-Trp-D-Ser-D-Phe(F5)-D-Cha-D-Arg-D-Arg-D-Arg-D-Gln-D-Arg-D-Arg-OH. CAS No. 565434-85-7. Molecular formula: C86H122F5N29O17. Mole weight: 1929.06.
CBP-93872
CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy. Synonyms: CBP 93872; CBP93872; 1-amino-3-((2-bromo-4-methylphenyl)amino)propan-2-ol. Grade: 98%. CAS No. 67427-51-4. Molecular formula: C10H15BrN2O. Mole weight: 259.14.
CBP-aminomethylenevancomycin
CBP-aminomethylenevancomycin is an analogue of vancomycin which overcomes the drug resistance and induces cell permeability. It significantly increases the antibacterial activity and decreases the side effects. Uses: Antibacterial agent. Synonyms: CBP aminomethylenevancomycin.
CBP-C1-aminomethylenevancomycin
CBP-C1-aminomethylenevancomycin is an analogue of vancomycin which overcomes the drug resistance and induces cell permeability. It significantly increases the antibacterial activity and decreases the side effects. Uses: Antibacterial agent. Synonyms: CBP C1 aminomethylenevancomycin.
CBP/EP300-IN-2
CBP/EP300-IN-2 is a CBP/EP300 inhibitor with IC50s of 1.07 and 5.96 nM for CBP/HTRF and Myc, respectively. (Extracted from patent WO2017205538A1, example 25). Synonyms: 5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[6-(difluoromethyl)-7-(1-methyl-1H-pyrazol-4-yl)-4-isoquinolinyl]-1,4,6,7-tetrahydro-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-; CBP/p300-IN-2; 3-[6-(Difluoromethyl)-7-(1-methyl-1H-pyrazol-4-yl)-4-isoquinolinyl]-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide. Grade: ≥95%. CAS No. 2158265-96-2. Molecular formula: C27H29F2N7O2. Mole weight: 521.56.
CBP-iminomethylenevancomycin
CBP-iminomethylenevancomycin is an analogue of vancomycin which overcomes the drug resistance and induces cell permeability. It significantly increases the antibacterial activity and decreases the side effects. Uses: Antibacterial agent. Synonyms: CBP iminomethylenevancomycin.
CBP/p300-IN-1
CBP/p300-IN-1 is an inhibitor of CBP/EP300 bromodomain. Synonyms: 2-Methyl-2-propanyl 3-{[(1-acetyl-5-methoxy-1H-indol-3-yl)carbonyl]amino}-4-fluorobenzoate; tert-Butyl 3-(1-acetyl-5-methoxy-1H-indole-3-carboxamido)-4-fluorobenzoate; Benzoic acid, 3-[[(1-acetyl-5-methoxy-1H-indol-3-yl)carbonyl]amino]-4-fluoro-, 1,1-dimethylethyl ester. Grade: ≥95%. CAS No. 2443789-32-8. Molecular formula: C23H23FN2O5. Mole weight: 426.44.
CBP/p300-IN-12
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 = 166 nM) and CBP inhibitor that reduces H3K27Ac levels in PC-3 cells (EC50 = 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450. Synonyms: N-(3-(3-((R)-3'-(2-((4-fluorobenzyl)((S)-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)ureido)phenyl)acrylamide. Molecular formula: C33H29F4N5O6. Mole weight: 667.61.
CBP/p300-IN-14
CBP/p300-IN-14 is a potent CBP/EP300 (lysine acetyltransferase) inhibitor with an IC50 of 3.3 nM. (Extracted from patent WO2021213521A1, compound 27). Synonyms: 3-Isoquinolinecarboxamide, 1-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-N-methyl-6-(4-methyl-2-oxo-1-piperazinyl)-; 1-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-N-methyl-6-(4-methyl-2-oxopiperazin-1-yl)isoquinoline-3-carboxamide. CAS No. 2725036-10-0. Molecular formula: C30H31F2N7O2. Mole weight: 559.61.
CBP/p300-IN-5
P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase with an IC50 of 18.8 nM. (Extracted from patent WO2016044770A1, Example 715). Synonyms: CBP/p300-IN-5; 2-[4-[(3'R,4S)-3'-fluoro-1-[2-[(4-fluorophenyl)methyl-[(1S)-2,2,2-trifluoro-1-methyl-ethyl]amino]-2-oxo-ethyl]-2,5-dioxo-spiro[imidazolidine-4,1'-indane]-5'-yl]pyrazol-1-yl]-N-methylacetamide; 2-((3'R,4S)-3'-Fluoro-5'-(1-(2-(methylamino)-2-oxoethyl)-1H-pyrazol-4-yl)-2,5-dioxo-2',3'-dihydrospiro[imidazolidine-4,1'-inden]-1-yl)-N-(4-fluorobenzyl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide; N-(4-Fluorobenzyl)-2-[(3'R,4S)-3'-fluoro-5'-{1-[2-(methylamino)-2-oxoethyl]-1H-pyrazol-4-yl}-2,5-dioxo-2',3'-dihydro-1H-spiro[imidazolidine-4,1'-inden]-1-yl]-N-[(2S)-1,1,1-trifluoro-2-propanyl]acetamide. Grade: ≥95%. CAS No. 1889284-33-6. Molecular formula: C29H27F5N6O4. Mole weight: 618.55.
CBP/p300-IN-8
CBP/p300-IN-8, a potent inhibitor of the CBP/P300 family of bromodomains, inhibits CBP and BRD4 activity with IC50s of 0.01-0.1 μM and 1-1000 μM, respectively. Synonyms: 6H-Imidazo[4,5-f]quinoline-6-carboxylic acid, 3-[(1S,3S)-3-carboxycyclohexyl]-3,7,8,9-tetrahydro-7-methyl-2-(phenylmethyl)-, 6-methyl ester, (7S)-; NSC-828853; (1S,3S)-3-[(7S)-2-Benzyl-6-(methoxycarbonyl)-7-methyl-6,7,8,9-tetrahydro-3H-imidazo[4,5-f]quinolin-3-yl]cyclohexanecarboxylic acid. Grade: ≥95%. CAS No. 2304416-91-7. Molecular formula: C27H31N3O4. Mole weight: 461.55.
CBR-470-1
CBR-470-1, a non-covalent Nrf2 activator, is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). It protects SH-SY5Y neuronal cells from MPP+ induced cytotoxicity by activating the Keap1-Nrf2 cascade. Synonyms: 3-Thiophenamine, 4-[(4-chlorophenyl)sulfonyl]tetrahydro-N-(2-methylpropyl)-, 1,1-dioxide, (3R,4S)-rel-; (3S,4R)-4-[(4-Chlorophenyl)sulfonyl]-N-isobutyltetrahydro-3-thiophenamine 1,1-dioxide; (3S,4R)-4-[(4-chlorophenyl)sulfonyl]-3-[(2-methylpropyl)amino]thiolane-1,1-dione. Grade: ≥98%. CAS No. 2416095-06-0. Molecular formula: C14H20ClNO4S2. Mole weight: 365.90.
CBR-470-2
CBR-470-2, an analogue of glycine substitution, activates NRF2 signaling and can be used to study modulation glycolysis. Synonyms: N-{(3S,4R)-4-[(3,4-Dichlorophenyl)sulfonyl]-1,1-dioxidotetrahydro-3-thiophenyl}glycine; Glycine, N-[(3R,4S)-4-[(3,4-dichlorophenyl)sulfonyl]tetrahydro-1,1-dioxido-3-thienyl]-, rel-. Grade: ≥95%. CAS No. 2416095-00-4. Molecular formula: C12H13Cl2NO6S2. Mole weight: 402.27.
CBR 5884
CBR 5884 is a 3-Phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50 = 33 μM), does not affect other NAD+-dependent dehydrogenases. Uses: 3-phosphoglycerate dehydrogenase (phgdh) inhibitor. Synonyms: CBR-5884; CBR 5884; CBR5884. Ethyl 5-[(2-furanylcarbonyl)amino]-3-methyl-4-thiocyanato-2-thiophenecarboxylate. Grade: ≥98%. CAS No. 681159-27-3. Molecular formula: C14H12N2O4S2. Mole weight: 336.39.
CBS1117
CBS1117 is an effective inhibitor of influenza A virus entry, which can inhibit influenza virus hemagglutinin. Synonyms: 2,6-Dichloro-N-[1-(Propan-2-Yl)Piperidin-4-Yl]Benzamide. Grade: 98%. CAS No. 959245-08-0. Molecular formula: C15H20Cl2N2O. Mole weight: 315.2.
CBS9106
CBS9106, also known as BMS-566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight. A reduced level of CRM1 protein is also observed in tumor xenografts isolated from mice treated with CBS9106. Taken together, these results indicate that CBS9106 is a novel reversible CRM1 inhibitor and a promising clinical candidate. Synonyms: SL-801; SL801; SL 801; CBS-9106; CBS 9106; BMS-566419; BMS566419; BMS 566419; 1H-Pyrrole-2,5-dione, 1-[[6-chloro-5-(trifluoromethyl)-2-pyridinyl]amino]-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-. Grade: 98%. CAS No. 1076235-04-5. Molecular formula: C18H21ClF3N3O3. Mole weight: 419.83.
CC0651
CC0651, a Cdc34 ubiquitin-conjugating enzyme allosteric inhibitor, has been found to restrain the cell proliferation at some extent in cancer cell lines PC-3. IC50: 1.72 uM (inhibited the ubiquitination of p27 Kip1). Uses: Cc0651 is a cdc34 ubiquitin-conjugating enzyme allosteric inhibitor that has been found to restrain the cell proliferation at some extent in cancer cell lines pc-3. ic50: 1.72 um (inhibited the ubiquitination of p27 kip1). Synonyms: CC0651; CC 0651; CC-0651; (2R,3S,4S)-5-[4-(3,5-dichlorophenyl)phenyl]-2,3-dihydroxy-4-[(2-methoxyacetyl)amino]pentanoicacid; CC0651; 1319207-44-7; 4,5-Dideoxy-5-(3',5'-Dichlorobiphenyl-4-Yl)-4-[(Methoxyacetyl)amino]-L-ArabinonicAcid; U94; SCHEMBL14884531. Grade: 95%. CAS No. 1319207-44-7. Molecular formula: C20H21Cl2NO6. Mole weight: 442.29.
CC-1088
CC-1088 is an analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). Uses: Cytokine inhibitor. Synonyms: CC1088; CC 1088; CC-1088. 3-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanamide. Grade: ≥98%. CAS No. 467421-06-3. Molecular formula: C17H14N2O3. Mole weight: 294.31.
CC-115
CC-115, a DNA-PK and mTOR inhibitor, has been found to have probable anticarcinoma effect. IC50:13 nM and 21 nM for DNA-PK and mTOR respectively. Uses: Cc-115 is a dna-pk and mtor inhibitor and has been found to have probable anticarcinoma effect. Synonyms: 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-5-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one; CC115 ; CC-115; CC 115. Grade: 98%. CAS No. 1228013-15-7. Molecular formula: C16H16N8O. Mole weight: 336.35.
CC-115 hydrochloride
The hydrochloride salt form of CC-115 which is a mTOR / DNA-PK inhibitor that probably has antineoplastic effect through influencing the cellular proliferation of cancer cells. IC50: 21 nM and 13 nM for mTOR and DNA-PK respectively. Uses: The hydrochloride salt form of cc-115 which is a mtor / dna-pk inhibitor that probably has antineoplastic effect through influencing the cellular proliferation of cancer cells. Synonyms: CC115 hydrochloride ; CC-115 hydrochloride; CC 115 hydrochloride. Grade: 98%. CAS No. 1300118-55-1. Molecular formula: C16H17ClN8O. Mole weight: 372.81.
CC-12074
A Metabolite of Pomalidomide. Uses: Pomalidomide metabolite. Synonyms: CC-12074; CC12074; CC 12074; Pomalidomide metabolite M19; UNII-A480CC1Z8I; SCHEMBL3742152.4-amino-2-(5-hydroxy-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione. Grade: ≥98%. CAS No. 460741-57-5. Molecular formula: C13H11N3O5. Mole weight: 289.24.
CC122
CC122 is a novel agent for DLBCL. It is an orally available pleiotropic pathway modulator. It has antitumor and immunomodulatory activity. It is used for the treatment of chronic lymphocytic leukemia. It binds CRBN and degrades Aiolos and Ikaros resulting in a mimicry of IFN signaling and apoptosis in DLBCL. It inhibits proliferation and induces apoptosis in ABC and GCB DLBCL in vitro. It was developed by Celgene Corporation(CELG) and was in clinic phase 2 trial. Uses: Cc122 has antitumor and immunomodulatory activity. it is used for the treatment of chronic lymphocytic leukemia. Synonyms: 3-(5-Amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione; CC-122; CC122; CC 122. Grade: >98 %. CAS No. 1015474-32-4. Molecular formula: C14H14N4O3. Mole weight: 286.29.
CC-17368
CC-17368 is a hydroxyisoindole derivative and metabolite of pomalidomide that has potential activity in anticancer study like multiple myeloma. Synonyms: CC 17368; CC17368; Pomalidomide metabolite M17; 1H-Isoindole-1,3(2H)-dione, 4-amino-2-(2,6-dioxo-3-piperidinyl)-5-hydroxy-. Grade: 98%. CAS No. 1547162-41-3. Molecular formula: C13H11N3O5. Mole weight: 289.25.
CC-17369
CC-17369, a hydroxyisoindole derivative, is a metabolites of pomalidomide and has potential activity in anticancer study like multiple myeloma. Synonyms: CC-17369; CC 17369; CC17369; Pomalidomide metabolite M16; M16(CC-17369); SCHEMBL15439588; 4-amino-2-(2,6-dioxopiperidin-3-yl)-7-hydroxyisoindole-1,3-dione. Grade: 98%. CAS No. 1547162-46-8. Molecular formula: C13H11N3O5. Mole weight: 289.25.
CC-223
CC-223, a mTOR kinase inhibitor, has been found to be effective in inducing the apoptosis and reducing the proliferation of tumor cells. It is still under Phase I/II clinical trial by Celgene Corporation. IC50: 16 nM. Uses: Cc-223 is a mtor kinase inhibitor that has been found to be effective in inducing the apoptosis and reducing the proliferation of tumor cells. Synonyms: CC-223; CC 223; CC223; UNII-I8RA3543SY; I8RA3543SY; 7-(6-(2-Hydroxypropan-2-yl)pyridin-3-yl)-1-(trans-4-methoxycyclohexyl)-3,4-dihydropyrazino(2,3-b)pyrazin-2(1H)-one; 7-(6-(2-Hydroxypropan-2-yl)pyridin-3-yl)-1-(trans-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyraz. Grade: 98%. CAS No. 1228013-30-6. Molecular formula: C21H27N5O3. Mole weight: 397.47.
CC-3052
CC-3052, a thalidomide analogue, reduces persistent activation of the TNF-α system in HIV without markedly impairing neutrophil viability. Synonyms: CC-3052; CC 3052; CC3052; methyl (2R)-2-(3,4-dimethoxyphenyl)-3-(3-oxo-1H-isoindol-2-yl)propanoate. Grade: >98%. CAS No. 216884-02-5. Molecular formula: C20H21NO5. Mole weight: 355.38.