CDK2: Small Molecules and Peptides
CDK2 (cyclin-dependent kinase 2), a serine/threonine protein kinase, is the catalytic subunit of the heterodimeric cyclin-dependent kinase complex required for G1/S phase transition. The kinase activity of CDK2 is regulated by the association with a cyclin subunit, CDK inhibitors, and its phosphorylation state. The active CDK2/cyclin A complex interacts with the N-terminus of E2F-1 and directs the phosphorylation of E2F-1 and DP-1. The active CDK2/cyclin E complex phosphorylates Rb which disrupts its binding to E2F, allowing E2F activation and transcription of the genes necessary for S-phase entry and progression. Inhibition of the CDK2/cyclin complex can be attributed to its association with p21Waf1/Cip1 and p27Kip1 and the phosphorylation of CDK2 on Thr14 and Tyr15. The activation of the CDK2/cyclin complex requires the phosphorylation of Thr160 and the dephosphorylation of Tyr14 and Tyr15.
18 results for "CDK2 Small Molecules and Peptides" in Products
18 results for "CDK2 Small Molecules and Peptides" in Products
CDK2: Small Molecules and Peptides
CDK2 (cyclin-dependent kinase 2), a serine/threonine protein kinase, is the catalytic subunit of the heterodimeric cyclin-dependent kinase complex required for G1/S phase transition. The kinase activity of CDK2 is regulated by the association with a cyclin subunit, CDK inhibitors, and its phosphorylation state. The active CDK2/cyclin A complex interacts with the N-terminus of E2F-1 and directs the phosphorylation of E2F-1 and DP-1. The active CDK2/cyclin E complex phosphorylates Rb which disrupts its binding to E2F, allowing E2F activation and transcription of the genes necessary for S-phase entry and progression. Inhibition of the CDK2/cyclin complex can be attributed to its association with p21Waf1/Cip1 and p27Kip1 and the phosphorylation of CDK2 on Thr14 and Tyr15. The activation of the CDK2/cyclin complex requires the phosphorylation of Thr160 and the dephosphorylation of Tyr14 and Tyr15.
HMG-CoA reductase inhibitor
| Chemical Name: | (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyly-2,2-dimethyl butanoate |
| Purity: | ≥98% (HPLC) |
Potent CDK2 inhibitor
| Alternate Names: | AUZ 454 |
| Chemical Name: | N-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea |
| Purity: | ≥98% (HPLC) |
Potent and selective inhibitor of CDK2, CDK5, CDK1 and CDK9
| Alternate Names: | SCH 727965 |
| Chemical Name: | (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol |
| Purity: | ≥98% (HPLC) |
Cdk inhibitor; potently inhibits cdk1 and cdk2
| Chemical Name: | (4-Butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl) (2,6-difluoro-4-methylphenyl)methanone |
| Purity: | ≥97% (HPLC) |
Cdk inhibitor; potently inhibits cdk2, cdk7 and cdk9
| Alternate Names: | BMS-387032 |
| Chemical Name: | N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide |
| Purity: | ≥98% (HPLC) |
Selective cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
| Alternate Names: | NG 95 |
| Chemical Name: | (2R)-2-[[6-[(3-Chloro-4-carboxyphenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol |
| Purity: | ≥98% (HPLC) |
Cdk2 and cdk5 inhibitor
| Chemical Name: | 2,2'-[[6-[[(4-Methoxyphenyl)methyl]amino]-9-(1-methylethyl)-9H-purin-2-yl]imino]bis[ethanol] |
| Purity: | ≥98% (HPLC) |
Potent and selective CDK2 Degrader (PROTAC®)
| Chemical Name: | 4-[[5-Amino-1-[(3-methyl-2-thienyl)carbonyl]-1H-1,2,4-triazol-3-yl]amino]-N-[2-[[1-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]benzenesulfonamide |
| Purity: | ≥98% (HPLC) |
Cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
| Alternate Names: | NG 60 |
| Chemical Name: | (2R)-2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol |
| Purity: | ≥98% (HPLC) |
Cdk inhibitor; potently inhibits cdk2 and cdk9
| Alternate Names: | L 86-8275 |
| Chemical Name: | 2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one hydrochloride |
| Purity: | ≥98% (HPLC) |
Potent and selective DYRK1A inhibitor
| Chemical Name: | 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole |
| Purity: | ≥98% (HPLC) |
Cdk inhibitor
| Alternate Names: | CYC 202,Seliciclib |
| Chemical Name: | (2R)-2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol |
| Purity: | ≥98% (HPLC) |
Potent HMG-CoA reductase inhibitor
| Alternate Names: | Mevinolin |
| Chemical Name: | (2S)-(1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl-2-methyl butanoate |
| Purity: | ≥97% (HPLC) |
Potent and selective cdk inhibitor; orally bioavailable
| Chemical Name: | [4-Amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)methanone |
| Purity: | ≥98% (HPLC) |
Cdk inhibitor; potently inhibits cdk1, 2, 5 and 9
| Chemical Name: | 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine |
| Purity: | ≥98% (HPLC) |
GSK-3β inhibitor; also inhibits cdks
| Chemical Name: | 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one |
| Purity: | ≥98% (HPLC) |
Potent covalent CDK14 and CDK16 inhibitor; also inhibits other TAIRE kinase family members
| Chemical Name: | N-[1-[[3-[[(2E)-4-(Dimethylamino)-1-oxo-2-buten-1-yl]amino]phenyl]sulfonyl]-4-piperidinyl]-4-[(2,4,6- trichlorobenzoyl)amino]-1H-pyrazole-3-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent cdk inhibitor
| Chemical Name: | 3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol |
| Purity: | ≥98% (HPLC) |
