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Activation of cyclin-dependentkinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependentkinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation. Group: Enzymes. Synonyms: Bur1; Bur1 Cdk; Cak1; Cak1p; cdc2; cdc2 kinase; Cdc28p; CDK; cdk-activating kinase; Cdk-activating protein kinase; cdk1; cdk2; Cdk2; cdk3; cdk4; cdk5; cdk6; cdk7; cdk8; cdk9; cyclin A-activated cdc2; cyclin A-activated cdk2; cyclin D-cdk6 kinase; cyclin D-depende. Enzyme Commission Number: EC 2.7.11.22. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3142; cyclin-dependentkinase; EC 2.7.11.22; Bur1; Bur1 Cdk; Cak1; Cak1p; cdc2; cdc2 kinase; Cdc28p; CDK; cdk-activating kinase; Cdk-activating protein kinase; cdk1; cdk2; Cdk2; cdk3; cdk4; cdk5; cdk6; cdk7; cdk8; cdk9; cyclin A-activated cdc2; cyclin A-activated cdk2; cyclin D-cdk6 kinase; cyclin D-dependentkinase; cyclin E kinase; cyclin-A associated kinase; cyclin-dependentkinase 6; cyclin-dependentkinase-2; cyclin-dependentkinase-4; cyclin-dependent protein kinase activating kinase; cyk; D-type cyclinkinase; nclk; neuronal cdc2-like kinase; PCTAIRE-1; STK25. Cat No: EXWM-3142.
10Z-Hymenialdisine
Insecticidal and cytotoxic. Potent NF-kappaB inhibitor. Inhibits various pro-inflammatory cytokines such as IL-1, IL-2, IL-6, IL-8, TNF-alpha and nitric oxide (NO) in a variety of cell lines. ATP-competitive kinase inhibitor. Inhibits DNA damage checkpoint at G2, cyclin-dependentkinases CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p25, GSK-3beta and casein kinase 1 (CK1). Potent mitogen-activated protein kinasekinase-1 (MEK-1) inhibitor. MARK (microtubule affinity-regulating kinase) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 500ug, 1mg. Molecular Formula: C??H??BrN?O?, Method for Determining. US Biological Life Sciences.
Isolated from sponge Axinella carteri. A potent inhibitor of mitogen-activated protein kinasekinase-1 (MEK-1) (IC50=6nm). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-b (GSK-3b) and CDK5/p35 in Alzheimers disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6uM), cyclin-dependentkinases CDK1/cyclin B (IC50=22nm), CDK2/cyclin A (IC50=70 nm), CDK2/cyclin E (IC50=40nm), CDK4/cyclin D1 (IC50 = 600nm), CDK5/p25 (IC50=28nm), GSK-3b (IC50=10nm), and casein kinase 1 (CK1) (IC50=35nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 250ug, 1mg. US Biological Life Sciences.
1-(2,3,5-Tri-O-benzoyl-b-D-ribofuranosyl)-5-Nitropyridine-2(1H)-One, a cyclin-dependentkinase 9 (CDK9) inhibitor, has exhibited a compelling potential against malignancies such as breast cancer, prostate cancer and multiple myeloma. It interferes with the propagation and fission of cancer-bearing cells, ultimately restraining the pathogenesis of the malady. This product has shown noteworthy efficacy in the discovery and evolution of progressive anti-tumor therapies whilst facilitating CDK9 inhibition`s related research undertakings. Synonyms: 5-nitro-1-(2',3',5'-tri-O-benzoyl-beta-ribofuranosyl)-2-pyridone; 5-nitro-1-(2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl)-2-pyridone; (2R,3R,4R,5R)-2-((Benzoyloxy)methyl)-5-(5-nitro-2-oxopyridin-1(2H)-yl)tetrahydrofuran-3,4-diyl dibenzoate; 2(1H)-Pyridinone, 5-nitro-1-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)-. Grades: ≥95%. CAS No. 59892-37-4. Molecular formula: C31H24N2O10. Mole weight: 584.53.
1- (3-Nitrophenyl) methanesulfonamide
1- (3-Nitrophenyl) methanesulfonamide is a useful synthetic intermediate. It can be used to synthesize synthesize disubstituted pyridine derivatives as inhibitors of the protein cyclin-dependentkinase (CDK). Group: Biochemicals. Grades: Highly Purified. CAS No. 110654-66-5. Pack Sizes: 500mg, 5g. Molecular Formula: C7H8N2O4S, Molecular Weight: 216.21. US Biological Life Sciences.
Worldwide
1,4-Bis(4-nitrophenyl)piperazine
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 1,4-Bis(4-nitrophenyl)piperazine; 16264-05-4; Piperazine, 1,4-bis(4-nitrophenyl)-EINECS 240-371-8UNII-P6TE7B2EYY. CAS No. 16264-05-4. Molecular formula: C16H16N4O4. Mole weight: 328.328.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 25. Grades: >95%. CAS No. 2488840-59-9. Molecular formula: C24H29N7O4. Mole weight: 479.54.
1-?(6-?Nitro-?3-?pyridinyl)?piperazine
1-?(6-?Nitro-?3-?pyridinyl)?piperazine is a reagent used in the preparation of highly potent and orally bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine cyclin-dependant kinases as anticancer agents. Also is an impurity of Palbociclib (P139900), an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 775288-71-6. Pack Sizes: 25mg, 50mg. Molecular Formula: C9H12N4O2. US Biological Life Sciences.
1-? (Benzyloxycarbonyl) ?pyrrolidine-?3-?carboxylic Acid is a reagent used in the synthesis of cyclin-dependentkinase 4-inhibitors (CDK4) for cancer treatments. Also used towards the discovery of a potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer pased upon benzimidazole carboxamide moieties. Group: Biochemicals. Grades: Highly Purified. CAS No. 188527-21-1. Pack Sizes: 100mg, 250mg. Molecular Formula: C13H15NO4, Molecular Weight: 249.26. US Biological Life Sciences.
Worldwide
1-Boc-4-(6-aminopyridin-3-yl)piperazine
1-Boc-4-(6-aminopyridin-3-yl)piperazine is used to prepare pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of cyclin-dependentkinases 4 and 6. Group: Biochemicals. Grades: Highly Purified. CAS No. 571188-59-5. Pack Sizes: 100mg, 250mg. Molecular Formula: C14H22N4O2. US Biological Life Sciences.
Worldwide
1-Boc-4-(6-aminopyridin-3-yl)piperazine-d4
1-Boc-4-(6-aminopyridin-3-yl)piperazine-d4 is an intermediate in synthesizing Palbociclib-d4 (P139901), an isotope labelled compound of Palbociclib (P139900). Palbociclib (P139900) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 1808106-94-6. Pack Sizes: 25mg, 50mg. Molecular Formula: C14H18D4N4O2. US Biological Life Sciences.
Worldwide
1-Piperazin-N-oxide Palbociclib
1-Piperazin-N-oxide Palbociclib is a derivative compound of Palbociclib (P139900). Palbociclib (also known as compound number PD-0332991) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C24H29N7O3, Molecular Weight: 463.53. US Biological Life Sciences.
Worldwide
2,6-Dichloro-9-isopropylpurine
Bohemine cyclin-dependentkinase inhibitor for the treatment of leukemia or other cancer. Group: Biochemicals. Alternative Names: 2,6-Dichloro-9-(1-methylethyl)-9H-purine. Grades: Highly Purified. CAS No. 203436-45-7. Pack Sizes: 250mg. US Biological Life Sciences.
2-? Chloro-? 8-? cyclopentyl-? 5-? methyl-? 8H-? pyrido [2, ? 3-? d] ? pyrimidin-? 7-? one is an impurity of Palbociclib (P139900),(also known as compound number PD-0332991) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 1013916-37-4. Pack Sizes: 250mg, 1g. Molecular Formula: C13H14ClN3O, Molecular Weight: 263.72. US Biological Life Sciences.
Worldwide
2-Chloro-9-methyl-6-(benzylamino)purine
2-Chloro-9-methyl-6-(benzylamino)purine is an intermediate in the synthesis of Olomoucine (O567000), a purine derivative which inhibits cyclin-dependentkinases and induces G1 arrest. Group: Biochemicals. Grades: Highly Purified. CAS No. 101622-53-1. Pack Sizes: 25mg, 250mg. Molecular Formula: C13H12ClN5. US Biological Life Sciences.
Worldwide
2-Chloro-9-methyl-6-(benzylamino)purine-d3
2-Chloro-9-methyl-6-(benzylamino)purine-d3 is an isotope labelled intermediate in the synthesis of Olomoucine (O567000), a purine derivative which inhibits cyclin-dependentkinases and induces G1 arrest. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg, 100mg. Molecular Formula: C13H9D3ClN5. US Biological Life Sciences.
Worldwide
2-Chloro-N-(phenylmethyl)-1H-purin-6-amine
2-Chloro-N-(phenylmethyl)-1H-purin-6-amine is an intermediate in the synthesis of Olomoucine (O567000), a purine derivative which inhibits cyclin-dependentkinases and induces G1 arrest. Group: Biochemicals. Grades: Highly Purified. CAS No. 39639-47-9. Pack Sizes: 100mg, 1g. Molecular Formula: C12H10ClN5. US Biological Life Sciences.
Worldwide
2-Iodoanisole
2-Iodoanisole is a useful synthetic intermediate. It can be used in the synthesis of piperidinyl diaminopyrimidines as cyclin-dependentkinase inhibitors with antitumor activity and polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth. Group: Biochemicals. Grades: Highly Purified. CAS No. 529-28-2. Pack Sizes: 10g, 25g. Molecular Formula: C7H7IO, Molecular Weight: 234.03. US Biological Life Sciences.
(2R,4aR,7R,8S,8aS)-7-(2-Amino-6-chloro-9H-purin-9-yl)-2-phenylhexahydropyrano[3,2-d][1,3]dioxin-8-ol, a potentially efficacious cancer therapeutic agent, remarkably impedes cyclin-dependentkinase 4/6 (CDK4/6) that are of paramount importance for the progress of cell cycle, thus exhibiting promising therapeutic potential for the remission of breast cancer as well as other types of malignancies. It has been extensively investigated that obstructing CDK4/6 activities effectively decelerates the malignant proliferation of cancerous cells which substantiates the validation of this therapeutic candidate. Synonyms: 2-(4-Amino-2-oxo-1(2H)-pyrimidinyl)-1,5-anhydro-2-deoxy-4,6-O-[(R)-phenylmethylene]-D-altritol. CAS No. 705967-79-9. Molecular formula: C18H18ClN5O4. Mole weight: 403.82.
3-Amino- Benzene methanesulfonamide
3-Amino- Benzene methanesulfonamide can be used to synthesize disubstituted pyridine derivatives as inhibitors of the protein cyclin-dependentkinase (CDK). Group: Biochemicals. Grades: Highly Purified. CAS No. 344750-15-8. Pack Sizes: 250mg, 2.5g. Molecular Formula: C7H10N2O2S, Molecular Weight: 186.23. US Biological Life Sciences.
Worldwide
3-ATA
3-ATA is a selective cyclin-dependentkinase 4 (CDK4) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 129821-08-5. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C13H10N2OS, Molecular Weight: 242.3. US Biological Life Sciences.
Worldwide
5-bromo-4-chloro-N-cyclopentylpyrimidin-2-amine
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 5-Bromo-4-chloro-N-cyclopentylpyrimidin-2-amine; 1823404-28-9; CS-0011349; D87404; 5-?Bromo-?4-?chloro-?N-?cyclopentylpyrimidin?-?2-?amine. CAS No. 1823404-28-9. Molecular formula: C9H11BrClN3. Mole weight: 276.56.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 27; Pyrido(2,3-d)pyrimidin-7(8H)-one, 6-acetyl-2-amino-8-cyclopentyl-5-methyl-. CAS No. 571189-64-5. Molecular formula: C15H18N4O2. Mole weight: 286.33.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 26; Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-. CAS No. 571189-51-0. Molecular formula: C25H31N7O2. Mole weight: 461.57.
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 4-[6-[(6-bromo-8-cyclopentyl-5-methyl-7-oxo-2-pyrido[2,3-d]pyrimidinyl)amino]-3-pyridinyl]-1-piperazinecarboxylic acid tert-butyl ester; tert-butyl 4-[6-[(6-bromo-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazine-1-carboxylate. CAS No. 571188-82-4. Molecular formula: C27H34BrN7O3. Mole weight: 584.51.
6-Bromotubercidin
6-Bromotubercidin, a formidable suppressor of cyclin-dependentkinases (CDKs) and adenosine kinase, extends its utility within the research of afflictions ranging from cancerous maladies, inflammatory agonies to neurophysiological perturbations. Synonyms: 8-Bromo-7-deazaadenosine; 6-Br-Tu; 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 6-bromo-7-beta-D-ribofuranosyl-. CAS No. 78000-56-3. Molecular formula: C11H13BrN4O4. Mole weight: 345.15.
6-Desacetyl-6-Bromo Palbociclib
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 6-Bromo-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one; Pyrido-[2,3-d]-pyrimidin-7-one 41. CAS No. 851067-56-6. Molecular formula: C22H26BrN7O. Mole weight: 484.402.
6-Desacetyl-6-Bromo Palbociclib Hydrochloride
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 6-bromo-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride. CAS No. 850918-83-1. Molecular formula: C22H27ClBrN7O. Mole weight: 520.86.
6-Desacetyl Palbociclib
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: Pyrido[2,3-d]pyriMidin-7(8H)-one, 8-cyclopentyl-5-Methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]aMino]-; Pyrido-[2,3-d]-pyrimidin-7-one 38. CAS No. 571190-22-2. Molecular formula: C22H27N7O. Mole weight: 405.506.
6-Desacetyl Palbociclib Hydrochloride
An impurity of Palbociclib, a selective inhibitor of cyclin-dependentkinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride. CAS No. 571189-66-7. Molecular formula: C22H28ClN7O. Mole weight: 441.96.
7-BIO
7-BIO is a derivative of indirubin that triggers a rapid cell death process that is distinct from apoptosis and devoid of cytochrome c release or caspase activation. Furthermore, in contrast to other indirubin derivatives, 7-BIO has only marginal activity against the classic indirubin targets, cyclin-dependentkinases and GSK3. Synonyms: 7-Bromoindirubin-3'-oxime; 7-bromo-3-(3-nitroso-1H-indol-2-yl)-1H-indol-2-ol. Grades: ≥99%. CAS No. 916440-85-2. Molecular formula: C16H10BrN3O2. Mole weight: 356.2.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependentkinases CDK4 and CDK6. Synonyms: Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-cyclopentyl-5-methyl-2,6-bis[[5-(1-piperazinyl)-2-pyridinyl]amino]; Palbociclib Impurity G. CAS No. 2458234-37-0. Molecular formula: C31H39N11O. Mole weight: 581.73.
ABC-1183
ABC-1183 is an inhibitor of glycogen synthase kinase 3 (GSK-3) alpha, glycogen synthase kinase 3 (GSK-3) beta and cyclindependentkinase 9 (CDK-9). It can induce cell apoptosis and various signaling pathways. ABC-1183 shows toxicity to many cell lines in humans and mice. Synonyms: ABC1183; ABC 1183; NSC797769; NSC-797769. Grades: > 99% by HPLC. CAS No. 1042735-18-1. Molecular formula: C18H14N4OS. Mole weight: 334.39.
Abemaciclib
Abemaciclib is a potent and selective inhibitor of cyclin-dependentkinases, CDK4 and CDK6, as a method to inhibit the proliferation of cancer cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 1231929-97-7. Pack Sizes: 5mg, 10mg. Molecular Formula: C27H32F2N8, Molecular Weight: 506.59. US Biological Life Sciences.
Worldwide
Abemaciclib
Abemaciclib is an orally available cyclin-dependentkinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: LY-2835219; LY 2835219; LY2835219; Verzenio; N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine. Grades: ≥98%. CAS No. 1231929-97-7. Molecular formula: C27H32F2N8. Mole weight: 506.61.
Abemaciclib-[d5]
Labelled Abemaciclib. Abemaciclib is an orally available cyclin-dependentkinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine-d5; N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine-d5. Grades: > 98%. CAS No. 1809251-51-1. Molecular formula: C27H27D5F2N8. Mole weight: 511.62.
Abemaciclib-[d7]
Labelled Abemaciclib. Abemaciclib is an orally available cyclin-dependentkinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine-d7. Grades: > 98%. Molecular formula: C27H25D7F2N8. Mole weight: 513.64.
AG-012917
AG-012917 is a broad spectrum cyclin-dependentkinase inhibitor with potential anticancer activity. Synonyms: AG 012917; AG012917; (S)-4-((4-amino-5-(2,6-difluorobenzoyl)thiazol-2-yl)amino)-N-((1-methylpyrrolidin-2-yl)methyl)benzamide. Grades: >98%. CAS No. 486414-16-8. Molecular formula: C23H23F2N5O2S. Mole weight: 471.52.
AG-012986
AG-012986 is a multitargeted cyclin-dependentkinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition,>83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. Synonyms: AG 012986; AG012986; Benzamide, 4-((4-amino-5-(2,6-difluorobenzoyl)-2-thiazolyl)amino)-N-((1R)-2-(dimethylamino)-1-methylethyl)-. Grades: >98%. CAS No. 486414-35-1. Molecular formula: C22H23F2N5O2S. Mole weight: 459.51.
AG-024104
AG-024104 is a broad spectrum cyclin-dependentkinase inhibitor with potential anticancer activity. Synonyms: AG 024104; AG024104. Grades: >98%. CAS No. 750575-23-6. Molecular formula: C24H28F2N6O4S2. Mole weight: 566.64.
Aloisine A
Aloisine a is a cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclindependentkinases (Cdks: IC50 =150nM, 120 nM, 400 nM and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively). Uses: A potent and selective cdk and gsk-3 inhibitor. Synonyms: Aloisine A;4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol. Grades: ≥98%. CAS No. 496864-16-5. Molecular formula: C16H17N3O. Mole weight: 267.33.
Alsterpaullone
Alsterpaullone is a potent glycogen synthase kinase-3 inhibitor and a potential therapeutic agent for the treatment of Parkinson disease. Alsterpaullone is also known as 9-Nitropaullone and NSC 705701, which is a derivative of kenpaullone and an ATP-competitive inhibitor of several cyclin-dependentkinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Alsterpaullone induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Alsterpaullone is a derivative of kenpaullone with slightly improved potency over kenpaullone, alsterpaullone selectively inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and GSK3α/β with IC50 values of 35, 15, 200, 40, and 4 nM, respectively. Synonyms: 9-Nitropaullone; NSC 705701; 7,12-Dihydro-9-nitro-indolo[3,2-d][1]benzazepin-6(5H)-one. Grades: ≥98%. CAS No. 237430-03-4. Molecular formula: C16H11N3O3. Mole weight: 293.3.
Alvocidib
Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependentkinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependentkinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. Uses: For research used only. Synonyms: Flavopiridol; HMR 1275. HMR1275. HMR-1275. Grades: 0.98. CAS No. 146426-40-6. Molecular formula: C21H20ClNO5. Mole weight: 401.84.
Aminopurvalanol A
Aminopurvalanol A is a selective, cell-permeable, reversible and ATP-competitive cyclin-dependentkinase (CDK) inhibitor. It is a 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties. It induces cell differentiation by preferentially targeting the G2/M-phase and acts intracellularly by inhibiting both Cdks and MAPKs. It potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 with IC50s values of 33, 33, 28, and 20 nM, respectively. It also inhibits growth of ovarian leukemic (SR), (IGROV1), colonic (KM12) and lung (NCI-H522) cells in antiproliferative assays in vitro. Synonyms: (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol; NG-97; NG97; NG 97; Aminopurvalanol A; Aminopurvalanol-A. Grades: ≥98% by HPLC. CAS No. 220792-57-4. Molecular formula: C19H26ClN7O. Mole weight: 403.91.
Aminopurvalanol A (NG97, (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol)
A cell-permeable, reversible and competitive inhibitor of cyclin-dependentkinases. IC50 values are: CDK1/cyclin B (33nm), CDK2/cyclin A (33nm), CDK2/cyclin E (28nm) and CDK5/p35 (20nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 220792-57-4. Pack Sizes: 1mg, 5mg . US Biological Life Sciences.
Worldwide
amsilarotene
Amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependentkinase (CDK) inhibitors, resulting in cell cycle arrest. Synonyms: TAC-101; TAC 101; TAC101; Am 555S; Benzoic acid, 4-[[3,5-bis(trimethylsilyl)benzoyl]amino]-. Grades: 99%. CAS No. 125973-56-0. Molecular formula: C20H27NO3Si2. Mole weight: 385.61.
Isolated from Streptomyces sp., Antibiotic UCN-01 inhibits protein kinase C (PKC) and cyclin-dependentkinase 2 (CDK2) resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these anti-cancer agents. Group: Biochemicals. Alternative Names: 7-Hydroxystaurosporine, UCN-01. Grades: Highly Purified. CAS No. 112953-11-4. Pack Sizes: 1mg. US Biological Life Sciences.
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Arcyriaflavin A
Arcyriaflavin A is a potent dual target agent of calcium/calmodulin-dependent protein kinase II (CaMKII) and cyclin-dependentkinase 4 (CDK4). Its IC50 values are 140 nM and 25 nM for CDK4 and CaMKII respectively, which is selective over protein kinase A (PKA) and PKC in vitro. It inhibits proliferation of HCT116 and NCI H460 human carcinoma cells and replication of human cytomegalovirus (HCMV) in vitro. It also inhibits proliferation and induces apoptosis of endometriotic cyst stromal cells (ECSCs). Synonyms: Arcyriaflavin A; Arcyriaflavin-A; 12,13-Dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione; 6,7,12,13-Tetrahydro-5H-Indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione; Maleimide Indolocarbazole. Grades: ≥98% by HPLC. CAS No. 118458-54-1. Molecular formula: C20H11N3O2. Mole weight: 325.32.
AT-7519
AT-7519 is an orally bioavailable small molecule CDK inhibitor with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclindependentkinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. Synonyms: AT-7519, AT7519, AT 7519, AT-7519 free base. Grades: 0.98. CAS No. 844442-38-2. Molecular formula: C16H17Cl2N5O2. Mole weight: 382.24.
AT7519 HCl
AT-7519 is an orally bioavailable small molecule CDK inhibitor with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclindependentkinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. Synonyms: AT7519 HCl; AT 7519 HCl; AT-7519 HCl. CAS No. 902135-91-5. Molecular formula: C16H18Cl3N5O2. Mole weight: 418.71.
AZD5438
AZD5438 is a potent inhibitor of cyclin-dependentkinase (cdk) 1, 2, and 9 (IC(50), 16, 6, and 20 nmol/L, respectively). Broad cdk inhibition may provide an effective method to impair the dysregulated cell cycle that drives tumorigenesis and AZD5438 has the pharmacologic profile that provides an ideal probe to test this premise. Synonyms: AZD5438; AZD-5438; AZD 5438. Grades: 0.98. CAS No. 602306-29-6. Molecular formula: C18H21N5O2S. Mole weight: 371.45664.
Bml-259
BML-259 is a potent cyclin-dependentkinase 5 (Cdk5) inhibitor, with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively. Group: Inhibitors. CAS No. 267654-00-2. Molecular formula: C14H16N2OS. Mole weight: 260.4. Appearance: White to off-white solid. Purity: >98%. IUPACName: 2-phenyl-N-(5-propan-2-yl-1,3-thiazol-2-yl)acetamide. Canonical SMILES: O=C(NC1=NC=C(C(C)C)S1)CC2=CC=CC=C2. Catalog: ACM267654002.
Bohemine
Bohemine, structurally similar to Olomoucine and Roscovitine, is a 2,6,9-trisubstituted purine derivative that inhibits cyclin-dependentkinases (CDKs) and exhibits anticancer activity. Synonyms: 3-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]propan-1-ol; 6-benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine; bohemine. Grades: ≥97%. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42.
Borrelidin (Treponemycin, U 78548, C2989)
Macrolide antibiotic. Bacterial and eukaryal threonyl-tRNA synthetase (THrRS) inhibitor. Antiangiogenic (IC50=0.8nM). Induces the collapse of formed capillary tubes in a dose-dependent fashion. In HUVECs, the capillary tube collapsing activity is mediated by the activation of caspases-3 and -8 and induction of apoptosis. Blocks the formation of spontaneous lung metastases of B16-BL6 melanoma cells. Cyclin-dependentkinase (CDK) inhibitor. Antiviral. Antimalarial. Group: Biochemicals. Grades: Highly Purified. CAS No. 7184-60-3. Pack Sizes: 500ug, 1mg, 5mg. US Biological Life Sciences.
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BSJ-Bump
BSJ-Bump is the negative control for BSJ-03-123. It displays binding and no degradation of cyclindependentkinases 6 (CDK6) in vitro. Synonyms: N-(2-(2-(2-(2-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)ethoxy)ethoxy)ethoxy)ethyl)-2-((2-(1-methyl-2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide. Grades: ≥98%. CAS No. 2409918-48-3. Molecular formula: C48H58N10O11. Mole weight: 951.05.
Butyrolactone I
Butyrolactone I is an exogenous inhibitor of CDK cyclin-dependentkinases. Group: Biochemicals. Grades: Highly Purified. CAS No. 87414-49-1. Pack Sizes: 200ug, 400ug. Molecular Formula: C24H24O7, Molecular Weight: 424.44. US Biological Life Sciences.
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Butyrolactone I
It is one of a family of three butyrolactones isolated from aspergillus fumigatus. It exhibits antitumor activity and inhibits the cell cycle at the G1/S and G2/M transitions. It is a selective inhibitor of cyclin-dependentkinases CDK1/cyclin B, CDK2 and CDK5. Synonyms: Olomoucin; 4'-O-Demethylversicolactone D; (2R)-2,5-Dihydro-4-hydroxy-2-[[4-hydroxy-3-(3-methyl-2-butenyl)phenyl]methyl]-3-(4-hydroxyphenyl)-5-oxo-2-furancarboxylic Acid Methyl Ester; (+)-3''-Dimethylallyl-butyrolactone II. Grades: >95% by HPLC. CAS No. 87414-49-1. Molecular formula: C24H24O7. Mole weight: 424.44.
CAY10554
Cyclin-dependentkinases (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. Grades: ≥95%. CAS No. 267654-00-2. Molecular formula: C14H16N2OS. Mole weight: 260.4.
CAY10574
Cyclin-dependentkinases (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. Grades: ≥95%. CAS No. 140651-18-9. Molecular formula: C9H10N6O. Mole weight: 218.2.
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-dependentkinase 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.
CDK1/2 Inhibitor III
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-dependentKinase 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-dependentKinase 1 Inhibitor. Grades: ≥95%. CAS No. 220749-41-7. Molecular formula: C17H11ClN2O. Mole weight: 294.7.
CDK2 Inhibitor II
The cyclin-dependentkinase 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-dependentkinase 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-dependentkinase 4/6 Inhibitor IV. Grades: ≥98%. CAS No. 359886-84-3. Molecular formula: C27H32N6O. Mole weight: 456.6.
CDK4-IN-1
CDK 4/6 Inhibitor is a part of a group of compounds that exhibits selective inhibitory properties towards Cyclin-DependentKinases 4 & 6. These compounds are most commonly used to treat patients with breast cancer. Synonyms: CDK4 IN 1; LEE011 analog; CDK4-IN-1; CDK4IN-1; CDK4-IN1; CDK4IN1; CDK4 IN 1; 4-[5-Chloro-3-(1-methylethyl)-1H-pyrazol-4-yl]-N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-2-pyrimidinamine. Grades: >98%. CAS No. 1256963-02-6. Molecular formula: C22H29ClN8. Mole weight: 440.97.
CDK9-IN-2
CDK9-IN-2 is a novel cyclin-dependentkinase 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.
CDK/CRK Inhibitor
CDK/CRK inhibitor is an inhibitor of cyclin-dependentkinases (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-dependentkinase 7 Inhibitor IV; Cyclin-dependentkinase/CDK-related kinase Inhibitor; RGB-286147; RGB 286147. Grades: ≥98%. CAS No. 784211-09-2. Molecular formula: C23H22Cl2N4O3. Mole weight: 473.4.
CGP74514A
CGP74514A is a cell permeable Cdk inhibitor selective for Cyclin-dependentkinase-1 (Cdk1) (IC50=25nM). CGP74514A was also reported also to affect the activities of other kinases including PKCα (IC50=6.1μM), PKA (IC50=125μM) and EGFR (IC50>10μM), but only at much higher concentrations. Synonyms: 2-N-[(1R,2S)-2-aminocyclohexyl]-6-N-(3-chlorophenyl)-9-ethylpurine-2,6-diamine; CGP 74514A; 481724-82-7 (CGP74514A HCl salt); CGP-74514A; CGP74514A; N(2)-(2-aminocyclohexyl)-N(6)-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine. Grades: >98%. CAS No. 190653-73-7. Molecular formula: C19H24ClN7. Mole weight: 385.9.
Debromohymenialdisine
Debromohymenialdisine (DBH) is a marine sponge alkaloid that inhibits Chk1 and Chk2, blocking G2 arrest. DBH also inhibits cyclin-dependentkinase 5/p25, protein tyrosine kinase 6, MAP kinasekinase 1, glycogen synthase kinase 3β and other kinases largely unrelated to DNA damage/repair and cell cycling. Synonyms: DBH; SKF 108753. Grades: ≥95%. CAS No. 75593-17-8. Molecular formula: C11H11N5O2. Mole weight: 245.2.
Dinaciclib
Cyclin-dependentkinases (CDKs) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. Dinaciclib inhibits CDK1, CDK2, CDK5, and CDK9 activity in vitro with IC50 values of 3, 1, 1, and 4 nM, respectively. Compared to the pan-CDK inhibitor flavopiridol, dinaciclib is an equally potent inhibitor of CDK1 and CDK9 but a 12-14-fold more potent inhibitor of CDK2 and CDK5. It has been shown to inhibit DNA synthesis by blocking thymidine incorporation in A2780 ovarian cancer cells with an IC50 value of 4nM. At 5mg/kg it prevents tumor growth by 50% in an A2780 ovarian carcinoma mouse xenograft model and is active against a broad spectrum of human tumor cell lines in vitro (IC50s = 7-17nM). Group: Biochemicals. Alternative Names: Sch 727965; (2S) -1- [3-Ethyl-7- [ [ (1-oxido-3-pyridinyl) methyl]amino]pyrazolo [1, 5-a]pyrimidin-5-yl]-2-piperidineethanol. Grades: Highly Purified. CAS No. 779353-01-4. Pack Sizes: 5mg. Molecular Formula: C21H28N6O2. US Biological Life Sciences.
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