CDK
CDK(细胞周期蛋白依赖性激酶)
CDKs (Cyclin-dependent kinases) are serine-threonine 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. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.
There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.
CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).
CDK 相关产品(269)
- GC11401Roscovitine (Seliciclib,CYC202)CAS: 186692-46-6纯度: >98.50% / >98.00%
Roscovitine (Seliciclib,CYC202)是一种有效的Cdk2/cyclin E抑制剂,IC 50 值为0.1μM。Roscovitine还抑制Cdk7/cyclin H、Cdk5/p35以及(cdc)/cyclin B,IC 50 值分别为0.49、0.16和0.65μM。
- GC11823LY2835219 free baseCAS: 1231929-97-7纯度: >99.50% / >97.00% / >99.00%
LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂,在非细胞实验中的 IC 50 分别为 2nM 和 10nM。
- GC12425CDK inhibitor IICAS: 1269815-17-9纯度: >98.50%
CDK inhibitor II 是一种有效且特异性的 CDK9 抑制剂,IC50 <8 nM,取自参考文献 1,实施例 4。
- GC12871CDK9 inhibitorCAS: 1415559-43-1纯度: >98.50%
CDK9 inhibitor 是一种新型的选择性 CDK9 抑制剂,用于治疗 HIV 感染,对 CDK9/CycT1 的 IC50 为 39 nM,从参考化合物 87 中提取。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC10840 | THZ1 | 1604810-83-4 | >98.50% | |
A covalent Cdk7 inhibitor | ||||
| GC10842 | LEE011 | 1211441-98-3 | >99.50% | |
LEE011是一种具有口服活性的特异性细胞周期蛋白依赖性激酶CDK4/6抑制剂。LEE011以纳摩尔浓度靶向cyclin D1/CDK4和cyclin D3/CDK6。 | ||||
| GC11022 | SB 218078 | 135897-06-2 | >98.00% | |
A potent Chk1 inhibitor | ||||
| GC11040 | Borrelidin | 7184-60-3 | >98.00% | |
An antiangiogenic antibiotic | ||||
| GC11324 | PHA-767491 | 845714-00-3 | - | |
A potent Cdc7 kinase inhibitor | ||||
| GC11396 | SNS-032 (BMS-387032) | 345627-80-7 | >99.00% | |
A Cdk2, Cdk7, and Cdk9 inhibitor | ||||
| GC11401 | Roscovitine (Seliciclib,CYC202) | 186692-46-6 | >98.50% / >98.00% | |
Roscovitine (Seliciclib,CYC202)是一种有效的Cdk2/cyclin E抑制剂,IC 50 值为0.1μM。Roscovitine还抑制Cdk7/cyclin H、Cdk5/p35以及(cdc)/cyclin B,IC 50 值分别为0.49、0.16和0.65μM。 | ||||
| GC11774 | KH CB19 | 1354037-26-5 | - | |
KH CB19 是一种有效的 CLK(cdc2 样激酶)抑制剂(CLK1 IC50\u003d19.7 nM;CLK3 IC50\u003d530 nM)。 | ||||
| GC11823 | LY2835219 free base | 1231929-97-7 | >99.50% / >97.00% / >99.00% | |
LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂,在非细胞实验中的 IC 50 分别为 2nM 和 10nM。 | ||||
| GC11971 | LY2857785 | 1619903-54-6 | >98.50% | |
A Cdk9 inhibitor | ||||
| GC12001 | BS-181 | 1092443-52-1 | - | |
A selective Cdk7 inhibitor | ||||
| GC12011 | P276-00 | 920113-03-7 | >98.00% | |
P276-00 (P276-00) 是一种有效的细胞周期蛋白依赖性激酶 (CDK) 抑制剂,可抑制 CDK9-cyclinT1、CDK4-cyclin D1 和 CDK1-cyclinB,IC50 分别为 20 nM、63 nM 和 79 nM。 P276-00 (P276-00) 对顺铂耐药细胞具有抗肿瘤活性。 | ||||
| GC12064 | SB1317 | 937270-47-8 | >99.50% | |
A multi-kinase inhibitor | ||||
| GC12348 | Ro 3306 | 872573-93-8 | >98.00% | |
Ro 3306是一种ATP竞争性抑制剂,主要靶向CDK1/cyclin B1(K i 值为35nmol/L)和CDK1/cyclin A复合物(K i 值为110nmol/L)。 | ||||
| GC12425 | CDK inhibitor II | 1269815-17-9 | >98.50% | |
CDK inhibitor II 是一种有效且特异性的 CDK9 抑制剂,IC50 <8 nM,取自参考文献 1,实施例 4。 | ||||
| GC12438 | AZD-5438 | 602306-29-6 | >99.50% | |
A potent inhibitor of CDKs | ||||
| GC12612 | JNJ-7706621 | 443797-96-4 | >99.50% | |
A dual inhibitor of CDKs and Aurora kinases | ||||
| GC12642 | THZ1 Hydrochloride | 1604810-83-4 | >98.00% | |
A covalent Cdk7 inhibitor | ||||
| GC12865 | BMS265246 | 582315-72-8 | >99.00% | |
A cell-permeable inhibitor of Cdk1 and Cdk2 | ||||
| GC12871 | CDK9 inhibitor | 1415559-43-1 | >98.50% | |
CDK9 inhibitor 是一种新型的选择性 CDK9 抑制剂,用于治疗 HIV 感染,对 CDK9/CycT1 的 IC50 为 39 nM,从参考化合物 87 中提取。 | ||||
| GC13328 | XL413 hydrochloride | 2062200-97-7 | >99.50% | |
A potent inhibitor of Cdc7 | ||||
| GC13511 | THZ2 | 1604810-84-5 | >99.50% | |
A Cdk7 inhibitor | ||||
| GC13690 | BS-181 HCl | 1397219-81-6 | >99.00% | |
A selective Cdk7 inhibitor | ||||
| GC13998 | AT7519 Hydrochloride | 902135-91-5 | >99.00% | |
A Cdk inhibitor | ||||
