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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. Grades: ≥98%. CAS No. 1243583-88-1. Molecular formula: C20H22O4. Mole weight: 326.4.
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. Grades: ≥98%. CAS No. 1268709-57-4. Molecular formula: C23H34N4O. Mole weight: 382.5.
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. Grades: ≥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. Grades: ≥98%. CAS No. 1542066-74-9. Molecular formula: C30H25BrFN5O. Mole weight: 570.5.
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. Grades: ≥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. Grades: ≥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. Grades: ≥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. Grades: ≥98%. CAS No. 1381846-21-4. Molecular formula: C16H19ClN4O2. Mole weight: 334.8.
CAY10704
Hepatitis C is a liver infection caused by the hepatitis C virus (HCV). It is a blood-borne virus, which can cause both acute and chronic hepatitis. CAY10704 is a potent inhibitor of hepatitis C virus (HCV) infection with EC50 of 17 nM. It displays good pharmacokinetics in mice with preferential liver distribution without significant hepatotoxicity. CAY10704 is also selective for HCV over dengue virus with EC50 of 4.62 μM. Synonyms: CAY 10704; CAY-10704. Grades: ≥98%. CAS No. 101784-44-5. Molecular formula: C18H20Cl2N2. Mole weight: 335.3.
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. Grades: ≥95%. CAS No. 1666171-29-4. Molecular formula: C41H54N6S2. Mole weight: 695.
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. Grades: ≥98%. CAS No. 848688-62-0. Molecular formula: C18H13N3O3S. Mole weight: 351.4.
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. Grades: ≥98%. CAS No. 388086-13-3. Molecular formula: C21H14Cl2N2O2. Mole weight: 397.3.
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.
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. Grades: >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. Grades: >98%. CAS No. 206275-15-2. Molecular formula: C26H22BrN5O2. Mole weight: 516.39.
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. Grades: ≥99%. CAS No. 913534-05-1. Molecular formula: C22H28ClN3O3. Mole weight: 417.93.
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. Grades: ≥98%. CAS No. 1150586-64-3. Molecular formula: C26H43NO3. Mole weight: 417.6.
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. Grades: ≥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. Grades: 98%. CAS No. 1379573-88-2. Molecular formula: C25H31N9O4. Mole weight: 521.57.
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. Grades: 98%. CAS No. 1379573-92-8. Molecular formula: C27H34N8O4. Mole weight: 534.61.
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. Grades: ≥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. Grades: ≥99% by HPLC. CAS No. 856702-40-4. Molecular formula: C21H19N3O2S.HCl. Mole weight: 413.92.
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. Grades: 98%. CAS No. 959245-08-0. Molecular formula: C15H20Cl2N2O. Mole weight: 315.2.
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. Grades: ≥98%. CAS No. 467421-06-3. Molecular formula: C17H14N2O3. Mole weight: 294.31.
CC4
CC4 is a selective α6β2 and α4β2 nAChR partial agonist (Ki = 12 and 26nM for rat α6β2 and α4β2 receptors, respectively). CC4 stimulates dopamine release from striatal slices in vitro, and attenuates nicotine-induced self-administration and conditional place preference in vivo. Synonyms: CC4; CC 4; CC-4; Alternine; Ethylenedi-cytisine; (1R,5S)-1,2,3,4,5,6-Hexahydro-3-[2-[(1R,5S)-1,5,6,8-tetrahydro-8-oxo-1,5-methano-2H-pyrido[1,2-a][1,5]diazocin-3(4H)-yl]ethyl]-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one. Grades: ≥98% by HPLC. CAS No. 492-02-4. Molecular formula: C24H30N4O2. Mole weight: 406.52.
CC-401
CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity. The activation of JNK signaling is indentified in many immune-mediated kidney disease models. Thus, as the JNK inhibitor, CC-401 is found to be effective in these renal injury models. Synonyms: CC-401; CC 401; CC401. Grades: >98%. CAS No. 395104-30-0. Molecular formula: C22H24N6O. Mole weight: 388.47.
CC 401 dihydrochloride
CC 401 dihydrochloride is a potent JNK inhibitor (Ki = 25-50 nM). CC 401 competitively binds to ATP-binding site of phosphorylated JNK to inhibit JNK. Uses: Hepatoprotective. Synonyms: CC-401 dihydrochloride; CC 401 dihydrochloride; CC401 dihydrochloride; 3-[3-[2-(1-Piperidinyl)ethoxy]phenyl]-5-(1H-1,2,4-triazol-5-yl)-1H-indazole dihydrochloride. Grades: ≥98% by HPLC. CAS No. 2250025-96-6. Molecular formula: C22H24N6O.2HCl. Mole weight: 461.39.
CC-401 hydrochloride
ATP-competitive, selective JNK inhibitor. Decreases c-Jun transcription activity and proliferation. Decreases cytochrome c release and caspase 3 activation. Shows anti-ischemic, anti-inflammatory and antiapoptotic effects in vivo. Synonyms: CC 401 hydrochloride; CC401 hydrochloride; CC401 HCl. Grades: >98%. CAS No. 1438391-30-0. Molecular formula: C22H25ClN6O. Mole weight: 424.93.
CC-618
CC-618 has been found to be a PPARβ/δ antagonist that could be used to study the potential biological activity of Cys249 at some extent. IC50: 10 μM. Synonyms: 5-Thiazolecarboxamide, 4-methyl-2-[4-(trifluoromethyl)phenyl]-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-; 4-Methyl-2-[4-(trifluoromethyl)phenyl]-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-5-thiazolecarboxamide; CC 618; CC618; 4-Methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-((5-(trifluoromethyl)pyridin-2-yl)sulfonyl)ethyl)thiazole-5-carboxamide. Grades: 98%. CAS No. 1680204-90-3. Molecular formula: C20H15F6N3O3S2. Mole weight: 523.47.
CC-90003
Extracellular-signal regulated kinases (ERKs) are a specific subtype of MAPK that have been extensively linked to regulation of synaptic plasticity and memory formation in many systems. CC-90003 is an irreversible and selective inhibitor of ERK1/2 with IC50s in the 10-20 nM range, which shows good kinase selectivity and antitumor activity in a 258-kinase biochemical assay. Synonyms: CC90003; CC 90003. Grades: ≥98%. CAS No. 1621999-82-3. Molecular formula: C22H21F3N6O2. Mole weight: 458.44.
CCCP
CCCP inhibits IFN-β production induced by various types of the STING pathway activators, and suppresses the phosphorylation of STING, TBK1, and IRF3 via disrupting the association of STING and TBK1. Synonyms: CCCP; Mesoxalonitrile 3-chlorophenylhydrazone; 2-[ (3-chlorophenyl) hydrazinylidene]propanedinitrile; Carbonyl Cyanide m Chlorophenyl Hydrazone; Carbonyl Cyanide m-Chlorophenyl; Hydrazone; Carbonyl Cyanide meta Chlorophenyl Hydrazone; Carbonyl Cyanide meta-Chlorophenyl Hydrazone; CCCP. CAS No. 555-60-2. Molecular formula: C9H5ClN4. Mole weight: 204.62.
CCMI
CCMI is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (nAChR). It was shown to induce positive modulation of acetylcholine (ACh)-induced EC5 currents (EC50 = 0.7 μM). CCMI enhances cognition in rodent models. Synonyms: AVL-3288; AVL 3288; AVL3288; XY-4083; XY 4083; XY4083; [N-(4-Chlorophenyl)]-α-[(4-chlorophenyl)-aminomethylene]-3-methyl-5-isoxazoleacetamide; (Z)-3-(4-chloroanilino)-N-(4-chlorophenyl)-2-(3-methyl-1,2-oxazol-5-yl)prop-2-enamide. CAS No. 917837-54-8. Molecular formula: C19H15Cl2N3O2. Mole weight: 388.25.
A potent CCR4 antagonist. Synonyms: C 021 dihydrochloride; C021 dihydrochloride; C-021 dihydrochloride; 2-(1,4'-Bipiperidine-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine; 2-(1,4'-Bipiperidin)-1'-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolinamine; C-021; CCR4 Antagonist; CHEMBL508207; 2-(1,4'-Bipiperidin)-1'-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolina. CAS No. 864289-85-0. Molecular formula: C27H41N5O2. Mole weight: 467.6.
CCR5 antagonist 1
CCR5 antagonist 1 is a CCR5 antagonist extracted from WO 2004054974 A2 that can inhibit HIV replication. Synonyms: AC-31371; HY-100261. Grades: >98%. CAS No. 716354-86-8. Molecular formula: C39H46ClF2N5O3S. Mole weight: 738.3.
CCT018159
CCT018159 is a novel inhibitor of heat shock protein (Hsp) 90 with potential anticancer activity. CCT018159 inhibited human Hsp90beta with comparable potency to 17-AAG and with similar ATP-competitive kinetics. The mean cellular GI(50) value of CCT018159 across a panel of human cancer cell lines, including melanoma, was 5.3 mumol/L. CCT018159 caused cell cytostasis associated with a G(1) arrest and induced apoptosis. CCT018159 also inhibited key endothelial and tumor cell functions implicated in invasion and angiogenesis. Synonyms: CCT-018159; CCT 018159. Grades: >98%. CAS No. 171009-07-7. Molecular formula: C20H20N2O4. Mole weight: 352.39.
CCT 031374 hydrobromide
CCT 031374 hydrobromide is an inhibitor of TCF-dependent transcription. It was shown to block BIO-induced β-catenin stabilization, and reduce nuclear and cytosolic β-catenin levels in mouse L-cells. Synonyms: SR 01000418274; CCT 031374 hydrobromide; SR01000418274; CCT031374 hydrobromide; SR-01000418274; CCT-031374 hydrobromide; 1-[1,1'-Biphenyl]-4-yl-2-(2,3-dihydro-9H-imidazo[1,2-a]benzimidazol-9-yl)ethanone hydrobromide. Grades: ≥98% by HPLC. CAS No. 1219184-91-4. Molecular formula: C23H19N3O.HBr. Mole weight: 434.33.
CCT128930
CCT128930 is a novel ATP-competitive AKT inhibitor discovered using fragment- and structure-based approaches. It is a potent, advanced lead pyrrolopyrimidine compound exhibiting selectivity for AKT over PKA, achieved by targeting a single amino acid difference. CCT128930 exhibited marked antiproliferative activity and inhibited the phosphorylation of a range of AKT substrates in multiple tumor cell lines in vitro, consistent with AKT inhibition. Synonyms: CCT128930; CCT-128930; CCT 128930. CAS No. 885499-61-6. Molecular formula: C18H20ClN5. Mole weight: 341.8379.
CCT129202
CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. CCT129202 significantly reversed ABCB1- and ABCG2-mediated MDR in vitro, in vivo and ex vivo by inhibiting the function of their transporters and enhanced the eradication of cancer stem-like cells by chemotherapeutic agents. CCT129202 may be a candidate as MDR reversal agent for antineoplastic combination therapy and merits further clinical investigation. Synonyms: CCT129202; CCT-129202; CCT 129202. CAS No. 942947-93-5. Molecular formula: C23H25ClN8OS. Mole weight: 497.02.
CCT-137690
CCT137690, an aurora kinase inhibitor CCT137690, is a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays and exhibits anti-proliferative activity against a wide range of human solid tumour cell lines. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis. This is accompanied by p53/p21/BAX induction, thymidine kinase 1 (TK1) downregulation and PARP cleavage. Furthermore, CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression. Importantly, in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation, this compound significantly inhibits tumour growth. The potent preclinical activity of CCT137690 suggests that this inhibitor may benefit patients with MYCN amplified neuroblastoma. Synonyms: CCT-137690. CCT 137690. CCT137690. CAS No. 1095382-05-0. Molecular formula: C26H31BrN8O. Mole weight: 551.48.
CCT196969
This active molecular is a novel , paradox-breaking pan-RAF inhibitor with anti-SRC activity and it blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK -ERK. CCT196969 also prevented growth of xenografts derived from patient tumours with resistance to BRAF and MEK inhibitors. Uses: Effective in drug-resistant braf mutant melanoma. Synonyms: CCT196969; CCT-196969; CCT 196969. N-[4-[(3,4-Dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-fluorophenyl]-N'-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]urea. Grades: 98%. CAS No. 1163719-56-9. Molecular formula: C27H24FN7O3. Mole weight: 513.52.
CCT241161
This active molecular is a novel , paradox-breaking pan-RAF inhibitor with anti-SRC activity and it blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK -ERK. CCT 241161 also prevented growth of xenografts derived from patient tumours with resistance to BRAF and MEK inhibitors. Uses: Effective in drug-resistant braf mutant melanoma. Synonyms: CCT241161; CCT-241161; CCT 241161. 1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-(methylthio)-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea. Grades: 98%. CAS No. 1163719-91-2. Molecular formula: C28H27N7O3S. Mole weight: 541.62.
CCT 241533 dihydrochloride
CCT 241533 dihydrochloride is a potent Chk2 inhibitor (IC50 = 3 nM) displaying >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. CCT 241533 inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells, and blocks ionizing radiation-induced apoptosis of mouse thymocytes. Synonyms: CCT 241533 dihydrochloride; CCT241533 dihydrochloride; CCT-241533 dihydrochloride; (3R,4S)-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-α,α-dimethyl-3-pyrrolidinemethanol dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1962925-28-5. Molecular formula: C23H27FN4O4.2HCl. Mole weight: 515.41.
CCT241736
CCT241736 is a potent and orally active and dual FLT3-Aurora inhibitor, which has IC50 values against FLT3, Aurora A and Aurora B of 0.035, 0.015 and 0.1 μM respectively. It also inhibits viability of the human FLT3-ITD positive AML cell lines MOLM-13 with 0.1 μM in cellular assay. Synonyms: CCT-241736; CCT 241736. Grades: ≥98%. CAS No. 1402709-93-6. Molecular formula: C22H23Cl2N7. Mole weight: 456.37.
CCT245737
CCT245737 is an orally bioactive CHK1 inhibitor (IC50 of 1.4 nM), displaying >1,000-fold selectivity against CHK2 and CDK1. It potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It causes inhibition of tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia. Synonyms: CCT-245737; CCT 245737; CCT245737; 5-[(4-{[(2R)-morpholin-2-ylmethyl]amino}-5-(trifluoromethyl)pyridin-2-yl)amino]pyrazine-2-carbonitrile. CAS No. 1489389-18-5. Molecular formula: C16H16F3N7O. Mole weight: 379.347.
CCT245737(S)
CCT245737, a nitrogen heterocycle compound, has been found to be a CHK1 inhibitor that could probable be effective in antineoplastic studies. It is still under Phase I trail for Solid tumours. IC50: 30-220 nM. Synonyms: CCT245737; CCT 245737; CCT-245737; GTPL9187; GTPL 9187; GTPL-9187; 5-[[4-[[(2R)-morpholin-2-yl]methylamino]-5-(trifluoromethyl)pyridin-2-yl]amino]pyrazine-2-carbonitrile. Grades: 98%. CAS No. 1489389-23-2. Molecular formula: C16H16F3N7O. Mole weight: 379.14.
CCT251545
CCT251545, a small molecule inhibitor of WNT signaling with oral activity, can be used as a selective chemical probe that exhibits >100-fold selectivity for the human Mediator complex-associated protein kinases CDK8 and CDK19 over 291 other kinases. IC50: Synonyms: 8-[3-chloro-5-[4-(1-methylpyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-oneCCT251545; CCT 251545; CCT-251545; CHEMBL34082138-(3-chloro-5-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one8-{3-Chloro-5-[4-(1-Methyl-1h-Pyrazol-4-Yl)ph. CAS No. 1661839-45-7. Molecular formula: C23H24ClN5O. Mole weight: 421.92.
CCT-251921
CCT-251921 has been found to be a CDK inhibitor that could be significant in the studies of colorectal cancer. Synonyms: CCT251921; CCT-251921; CCT 251921; 8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one. Grades: 98%. CAS No. 1607837-31-9. Molecular formula: C21H23ClN6O. Mole weight: 410.91.
CCX140-B
CCX140-B is a potent CCR2 antagonist. Synonyms: CCX140; Ilacirnon. CAS No. 1100318-47-5. Molecular formula: C20H13ClF3N5O3S. Mole weight: 495.9.
CD 2314
CD 2314 is a potent and selective RARβ receptor agonist (Kd = 145 and >3760 nM for RARβ and RARα receptors, respectively). Synonyms: CD-2314; CD 2314; CD2314; 5-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-anthracenyl)-3-thiophenecarboxylic acid. Grades: ≥98% by HPLC. CAS No. 170355-37-0. Molecular formula: C23H24O2S. Mole weight: 364.5.
CD 2665
CD 2665 is a selective RARβ and RARγ antagonist (KD = 110, 306 and > 1000 nM for RARγ, RARβ and RARα respectively) with no activity at RXR&alpha. CD 2665 is used to abrogate retinoic acid-induced apoptosis, proliferation and differentiation of sebocyte growth. Synonyms: CD2665; CD 2665; CD-2665. 4-[6-[(2-Methoxyethoxy)methoxy]-7-tricyclo[3.3.1.13,7]dec-1-yl-2-naphthalenyl)benzoic acid. Grades: ≥98% by HPLC. CAS No. 170355-78-9. Molecular formula: C31H34O5. Mole weight: 486.6.
CD 3254
CD 3254 is a selective RXRα agonist with no activity at RARα, RARβ or RARγ receptors. Synonyms: CD3254; CD 3254; CD-3254. 3-[4-Hydroxy-3-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)phenyl]-2-propenoic acid. Grades: ≥97% by HPLC. CAS No. 196961-43-0. Molecular formula: C24H28O3. Mole weight: 364.48.
CDC801
A potent, orally active and dual inhibitor of phosphodiesterase 4 (PDE4) (IC50= 1.1 μM) and tumor necrosis factor-α (TNF-α) (IC50= 2.5 μM). Synonyms: CDC801; CDC 801; CDC-801; 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-(1,3-dioxoisoindol-2-yl)propanamide. CAS No. 192819-27-5. Molecular formula: C23H24N2O5. Mole weight: 408.45.
CDD0102
CDD0102 is a selective M1 agonist which stimulated the secretion of APP from CHO-K1 cells expressing M1 receptors and penetrated into the brain following i.p. administration in rodents. Synonyms: CDD0102; CDD 0102; CDD-0102; 3-ethyl-5-(1,4,5,6-tetrahydropyrimidin-5-yl)-1,2,4-oxadiazole; 5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine; CDD-0102A. CAS No. 146422-58-4. Molecular formula: C8H12N4O. Mole weight: 180.21.
CDDO-DhTFEA
CDDO-DhTFEA can effectively activate Nrf2 and inhibit the pro-inflammatory transcription factor NF-κB. Synonyms: RTA Dh404; RTA Dh404RTA Dh404. CAS No. 1191265-33-4. Molecular formula: C33H45F3N2O3. Mole weight: 574.7.
CDDO-EA
CDDO-EA is an activator of Nrf2/ARE. It has neuroprotective effect. Synonyms: CDDO ethyl amide; RTA405; TP319; RTA 405; TP 319; RTA-405; TP-319. Grades: >98%. CAS No. 932730-51-3. Molecular formula: C33H46N2O3. Mole weight: 518.73.
CDIBA
CDIBA is a potent and selective cytosolic phospholipase A2 (cPLA2) inhibitor. Synonyms: 4-[2-(1-benzhydryl-5-chloro-2-methylindol-3-yl)ethoxy]benzoic acid. Grades: 99%. CAS No. 479422-22-5. Molecular formula: C31H26ClNO3. Mole weight: 496.
Cdk1/2 Inhibitor III is a selective inhibitor of Cdk1/2 with an IC50 of 2.1 μM for CDK1/cyclin B. It is a cell-permeable triazolo-diamine compound with anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa and A375 cells, respectively). Synonyms: Cyclin-dependent Kinase 1/2 Inhibitor III; 1H-1,2,4-Triazole-1-carbothioamide, 3-amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-; 3-Amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide; 3-amino-N-(2,6-difluorophenyl)-5-((4-sulfamoylphenyl)amino)-1H-1,2,4-triazole-1-carbothioamide. Grades: >95%. CAS No. 443798-55-8. Molecular formula: C15H13F2N7O2S2. Mole weight: 425.44.
CDK1 Inhibitor
Cdk1 inhibitor is a cell-permeable indolylmethylene-2-indolinone derivative that exhibits potent anti-proliferative properties with IC50 of 2 μM. Cdk1 inhibitor acts as a selective and ATP-competitive inhibitor of Cdk1/cyclin B with IC50 of 5.8 μM. It also inhibits Cdk5 with IC50 of 25 μM. Synonyms: Cyclin-dependent Kinase 1 Inhibitor. Grades: ≥95%. CAS No. 220749-41-7. Molecular formula: C17H11ClN2O. Mole weight: 294.7.
CDK2 Inhibitor II
The cyclin-dependent kinase 2 (Cdk2) works with cyclins A or E to regulate S phase and G2-M transition during the cell cycle. Cdk2 Inhibitor II is a potent, cell-permeable, ATP-competitive, and selective inhibitor of Cdk2. It is a 3-(benzylidne)indolin-2-one analog that selectively and potently inhibits Cdk2 with IC50 of 60 nM. Synonyms: Cyclin-dependent kinase 2 Inhibitor II; SC-221409. Grades: ≥95%. CAS No. 222035-13-4. Molecular formula: C14H11BrN4O3S. Mole weight: 395.2.
CDK4/6 Inhibitor IV
Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 with IC50 values of 1.5 μM and Cdk6/cyclin D1 with IC50 values of 5.6 μM. It exhibits blocking of pRb phosphorylation at Ser780 and Ser795. Cdk4/6 inhibitor IV can suppresses tumor growth in Xenograft mouse model. Synonyms: CINK4; Cyclin-dependent kinase 4/6 Inhibitor IV. Grades: ≥98%. CAS No. 359886-84-3. Molecular formula: C27H32N6O. Mole weight: 456.6.
CDK4 Inhibitor
Cdk4 inhibitor is a cell-permeable, asymmetrical indolocarbazole that exhibits antiproliferative activity by blocking cyclin D1/Cdk4 with an IC50 of 0.8 μM. It also inhibits the activity of other Cdk's only at much higher concentrations (IC50 = 520 nM and 2.1 μM for Cdk2/E and Cdk1/B, respectively). Cdk4 inhibitor can inhibit tumor cells growth in HCT-116 and NCI-H460 cells (IC50 < 3.0 μM). Synonyms: 2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione. Grades: ≥90%. CAS No. 546102-60-7. Molecular formula: C20H10BrN3O2. Mole weight: 404.22.
CDK9-IN-1
Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays. Synonyms: CDK9-IN-1; CDK9 IN 1. Grades: >98%. CAS No. 1415559-43-1. Molecular formula: C26H21N5O4S. Mole weight: 499.54.
CDK9-IN-2
CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor. Synonyms: CDK9 Inhibitor II; CDK9 Inhibitor 2; CDK9-In-2; CDK9-IN2. Grades: >98%. CAS No. 1263369-28-3. Molecular formula: C23H25ClFN5. Mole weight: 425.93.
CDK9-IN-6
CDK9-IN-6, one of the CDK9 inhibitors, probably have potential activity in influencing cell cycle of T-type cells. Uses: Cdk9-in-6 is one of the cdk9 inhibitors that probably have potential activity in influencing cell cycle of t-type cells. Synonyms: CDK9-IN-6; SCHEMBL12466375; SCHEMBL15378321; SCHEMBL15378323; CS-4615; CS 4615; CS4615. Grades: 98%. CAS No. 1391855-95-0. Molecular formula: C27H37ClN6O2. Mole weight: 513.08.
CDK/CRK Inhibitor
CDK/CRK inhibitor is an inhibitor of cyclin-dependent kinases (CDK) and CDK-related kinases (CRK) with IC50 values ranging from 9-839 nM. It is also a potent, selective & ATP-competitive inhibitor of CDKs. CDK/CRK inhibitor exhibits less than 20% inhibition of 60 non-CDK/CRK kinases at 1 μM. Synonyms: Cdk7 Inhibitor IV; Cyclin-dependent kinase 7 Inhibitor IV; Cyclin-dependent kinase/CDK-related kinase Inhibitor; RGB-286147; RGB 286147. Grades: ≥98%. CAS No. 784211-09-2. Molecular formula: C23H22Cl2N4O3. Mole weight: 473.4.
CDKI-73
CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a mean LD50 value of 0.08μM ± 0.10 μM following exposure to drug for 48h. In contrast, normal B-lymphocytes (n = 10) and CD34+ normal bone marrow cells (n = 5) were significantly less susceptible to the cytotoxic effects of CDKI-73. Treatment of CLL cells with 0.1 μM CDKI-73 for 4h inhibited the phosphorylation of cdk9 and ser2 of RNA polymerase II. CDKI-73 induces a rapid loss of MCL1 protein and this is mediated by significant inhibition at the level of gene transcription. However, this inhibition is not restricted to MCL1 as similar reductions in XIAP and CCND2 were also observed following exposure to CDKI-73 for 4h. CDKI-73 rapidly inhibited cellular CDK9 kinase activity and down-regulated the RNAPII phosphorylation. CDK9 shRNA was also found to down-regulate the Mnk1 expression. Both CDKI-73 and CDK9 shRNA decreased anti-apoptotic proteins Mcl-1 and Bcl-2 and induced apoptosis. CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F=56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice. Synonyms: CDKI-73; CDKI 73; CDKI73. Grades: >98%. CAS No. 1421693-22-2. Molecular formula: C15H15FN6O2S2. Mole weight: 394.45.
CDK-IN-2
CDK-IN-2 is a potent and sepecific CDK inhibitor. Synonyms: CDK inhibitor II. Grades: >98%. CAS No. 1269815-17-9. Molecular formula: C18H19ClFN3O2. Mole weight: 363.81.
CDPPB
CDPPB is a positive allosteric modulator of mGlu5 receptor (EC50 = 10 and 20 nM for human and rat receptors, respectively). Study shows that CDPPB has a therapeutic effect for cognitive deficits in schizophrenia and pathology in Huntington's disease. CDPPB is a potential antipsychotic and nootropic drug. Synonyms: 3-Cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide; 3-cyano-N-(2,5-diphenylpyrazol-3-yl)benzamide. Grades: ≥98% by HPLC. CAS No. 781652-57-1. Molecular formula: C23H16N4O. Mole weight: 364.4.