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)
- GC14987GSK-3 Inhibitor IX (BIO)CAS: 667463-62-9纯度: >99.50%
GSK-3 Inhibitor IX (BIO)是一种强效、选择性和可逆的糖原合成酶激酶-3(GSK-3)抑制剂,对GSK-3α/β的IC 50 值为5nM。
- GC15377LEE011 succinateCAS: 1374639-75-4纯度: >99.50%
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor
- GC15421Palbociclib (PD0332991) IsethionateCAS: 827022-33-3纯度: >99.50% / >98.00%
Palbociclib (PD 0332991) isethionate 是一种具有口服活性的选择性 CDK4 和 CDK6 抑制剂,IC50 值分别为 11 和 16 nM。 Palbociclib (PD0332991) Isethionate 具有有效的抗增殖活性,可诱导癌细胞的细胞周期停滞,可用于 HR 阳性和 HER2 阴性乳腺癌和肝细胞癌的研究。
- GC15597AT7519 trifluoroacetateCAS: 1431697-85-6纯度: >98.00%
AT7519 (AT7519M) TFA 作为一种有效的 CDK 抑制剂,对 CDK1、CDK2、CDK4 到 CDK6 和 CDK9 的 IC50 分别为 210、47、100、13、170 和 <10 nM。
- GC15922LEE011 hydrochlorideCAS: 1211443-80-9纯度: >98.00%
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor
- GC16425Flavopiridol hydrochlorideCAS: 131740-09-5纯度: >98.00%
An inhibitor of cyclin-dependent kinases
- GC16959NVP-LCQ195CAS: 902156-99-4纯度: >99.50%
NVP-LCQ195 (AT9311; LCQ195) 是 CDK1、CDK2、CDK3 和 CDK5 的小分子杂环抑制剂,IC50 为 1-42 nM。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC14162 | ML167 | 1285702-20-6 | >98.50% | |
A selective Clk4 inhibitor | ||||
| GC14182 | Kenpaullone | 142273-20-9 | >98.00% | |
A inhibitor of cyclin-dependent kinase and GSK3β | ||||
| GC14230 | K03861 | 853299-07-7 | >98.00% | |
K03861 (K03861) 是一种 II 型 CDK2 抑制剂,Kd 为 8.2 nM。 K03861 (K03861) 通过与活化细胞周期蛋白的结合竞争抑制 CDK2 活性。 | ||||
| GC14707 | Purvalanol A | 212844-53-6 | >99.00% | |
A selective inhibitor of cyclin-dependent kinases | ||||
| GC14974 | AMG 925 | 1401033-86-0 | >98.00% | |
A dual inhibitor of FLT3 and Cdk4 | ||||
| GC14987 | GSK-3 Inhibitor IX (BIO) | 667463-62-9 | >99.50% | |
GSK-3 Inhibitor IX (BIO)是一种强效、选择性和可逆的糖原合成酶激酶-3(GSK-3)抑制剂,对GSK-3α/β的IC 50 值为5nM。 | ||||
| GC15047 | PHA-793887 | 718630-59-2 | >98.00% | |
A CDK inhibitor | ||||
| GC15377 | LEE011 succinate | 1374639-75-4 | >99.50% | |
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor | ||||
| GC15421 | Palbociclib (PD0332991) Isethionate | 827022-33-3 | >99.50% / >98.00% | |
Palbociclib (PD 0332991) isethionate 是一种具有口服活性的选择性 CDK4 和 CDK6 抑制剂,IC50 值分别为 11 和 16 nM。 Palbociclib (PD0332991) Isethionate 具有有效的抗增殖活性,可诱导癌细胞的细胞周期停滞,可用于 HR 阳性和 HER2 阴性乳腺癌和肝细胞癌的研究。 | ||||
| GC15571 | SU 9516 | 377090-84-1 | >99.50% | |
A pro-apoptotic Cdk2/cyclin A inhibitor | ||||
| GC15588 | PHA-848125 | 802539-81-7 | >99.50% | |
An inhibitor of Cdks | ||||
| GC15597 | AT7519 trifluoroacetate | 1431697-85-6 | >98.00% | |
AT7519 (AT7519M) TFA 作为一种有效的 CDK 抑制剂,对 CDK1、CDK2、CDK4 到 CDK6 和 CDK9 的 IC50 分别为 210、47、100、13、170 和 <10 nM。 | ||||
| GC15607 | ON123300 | 1357470-29-1 | >99.00% | |
A multi-kinase inhibitor | ||||
| GC15841 | Alsterpaullone | 237430-03-4 | >98.00% | |
A dual CDK and GSK3 inhibitor | ||||
| GC15870 | AT7519 | 844442-38-2 | >99.50% | |
A Cdk inhibitor | ||||
| GC15922 | LEE011 hydrochloride | 1211443-80-9 | >98.00% | |
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor | ||||
| GC16063 | Flavopiridol | 146426-40-6 | >98.00% | |
An inhibitor of cyclin-dependent kinases | ||||
| GC16268 | Purvalanol B | 212844-54-7 | >98.50% | |
A CDK inhibitor | ||||
| GC16420 | THZ531 | 1702809-17-3 | >98.00% | |
An inhibitor of Cdk12 and Cdk13 | ||||
| GC16425 | Flavopiridol hydrochloride | 131740-09-5 | >98.00% | |
An inhibitor of cyclin-dependent kinases | ||||
| GC16511 | OTS964 | 1338545-07-5 | >99.00% | |
A TOPK inhibitor | ||||
| GC16822 | LY2835219 | 1231930-82-7 | >99.00% | |
LY2835219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。 | ||||
| GC16959 | NVP-LCQ195 | 902156-99-4 | >99.50% | |
NVP-LCQ195 (AT9311; LCQ195) 是 CDK1、CDK2、CDK3 和 CDK5 的小分子杂环抑制剂,IC50 为 1-42 nM。 | ||||
| GC17067 | LDC000067 | 1073485-20-7 | >98.50% | |
A Cdk9 inhibitor | ||||
