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)
- GC37529Ribociclib succinate hydrateCAS: 1374639-79-8纯度: >99.50%
Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
- GC38377(2S,3R)-Voruciclib hydrochloride纯度: >98.00%
(2S,3R)-Voruciclib hydrochloride 是 Voruciclib hydrochloride 的低活性异构体。Voruciclib hydrochloride 是一种 CDK9 抑制剂。
- GC38749Abemaciclib metabolite M20CAS: 2138499-06-4纯度: >98.00%
Abemaciclib metabolite M20 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂，可用于癌症的相关研究
- GC38899CDK ligand for PROTAC hydrochloride
CDK ligand for PROTAC hydrochloride 是一种具有抗肿瘤活性的 CDK 抑制剂。CDK ligand for PROTAC hydrochloride 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。
- GC39162TCMDC-135051CAS: 2413716-15-9
TCMDC-135051 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂，具有低的靶外毒性。TCMDC-135051 可以防止滋养体到裂殖体的转变，破坏转录并减少向蚊子载体的传播。TCMDC-135051 具有抗寄生虫活性 (EC50=320 nM)。
- GC39175SR-4835CAS: 2387704-62-1纯度: >99.50%
SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.
- GC39421PNU112455A hydrochlorideCAS: 21886-12-4纯度: >98.00%
PNU112455A hydrochloride是CDK2和CDK5的ATP位点的竞争性抑制剂，其对CDK2和CDK5中ATP位点的Km值分别为3.6μM和3.2μM。
- GC40092PD 0332991-d8CAS: 1628752-83-9纯度: >99.50%
An internal standard for the quantification of PD 0332991
- GC50217BS 181 dihydrochlorideCAS: 1883548-83-1
BS 181 dihydrochloride 是一种比 Seliciclib 有效且选择性的 CDK7 抑制剂 (IC50\u003d21 nM)。 BS-181 还针对 CDK2、CDK5 和 CDK9，IC50 值分别为 880 nM、3000 nM 和 4200 nM（无法阻断 CDK1、4 和 6）。 BS 181 dihydrochloride 抑制一组癌细胞生长 (IC50\u003d11.5 μM-37.3 μM) 并诱导细胞凋亡。 BS 181 dihydrochloride 具有研究癌症治疗的潜力。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC37522 | RGB-286638 | 784210-87-3 | >99.50% | |
A multi-kinase inhibitor | ||||
| GC37523 | RGB-286638 free base | 784210-88-4 | - | |
A multi-kinase inhibitor | ||||
| GC37529 | Ribociclib succinate hydrate | 1374639-79-8 | >99.50% | |
Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. | ||||
| GC37627 | Senexin A | 1366002-50-7 | >99.50% | |
Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively. | ||||
| GC37709 | SY-1365 | 1816989-16-8 | >99.00% | |
SY-1365 (SY-1365) 是一种有效的一流的选择性 CDK7 抑制剂，Ki 为 17.4 nM。 SY-1365 在实体瘤细胞系中表现出抗增殖和凋亡作用。 SY-1365 在血液学和多种侵袭性实体瘤中具有抗肿瘤活性。 | ||||
| GC37786 | THZ1-R | 1621523-07-6 | >98.00% | |
A non-cysteine reactive derivative of THZ1 | ||||
| GC38330 | EHT 5372 | 1425945-60-3 | - | |
EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，其 IC50 值分别为 0.22，0.28 nM。 | ||||
| GC38377 | (2S,3R)-Voruciclib hydrochloride | - | >98.00% | |
(2S,3R)-Voruciclib hydrochloride 是 Voruciclib hydrochloride 的低活性异构体。Voruciclib hydrochloride 是一种 CDK9 抑制剂。 | ||||
| GC38482 | Desmethylglycitein | 17817-31-1 | - | |
An active metabolite of daidzein | ||||
| GC38736 | AS2863619 | 2241300-51-4 | >98.00% | |
AS2863619是一种口服小分子环依赖性激酶（CDK）8和19抑制剂，IC 50 值分别为0.6099nM和4.277nM。 | ||||
| GC38737 | AS2863619 free base | 2241300-50-3 | >98.00% | |
A dual inhibitor of Cdk8 and Cdk19 | ||||
| GC38749 | Abemaciclib metabolite M20 | 2138499-06-4 | >98.00% | |
Abemaciclib metabolite M20 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂，可用于癌症的相关研究 | ||||
| GC38755 | CKI-7 | 120615-25-0 | >99.00% | |
A CK1 inhibitor | ||||
| GC38899 | CDK ligand for PROTAC hydrochloride | - | - | |
CDK ligand for PROTAC hydrochloride 是一种具有抗肿瘤活性的 CDK 抑制剂。CDK ligand for PROTAC hydrochloride 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。 | ||||
| GC39162 | TCMDC-135051 | 2413716-15-9 | - | |
TCMDC-135051 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂，具有低的靶外毒性。TCMDC-135051 可以防止滋养体到裂殖体的转变，破坏转录并减少向蚊子载体的传播。TCMDC-135051 具有抗寄生虫活性 (EC50=320 nM)。 | ||||
| GC39175 | SR-4835 | 2387704-62-1 | >99.50% | |
SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. | ||||
| GC39281 | (R)-CR8 trihydrochloride | 1786438-30-9 | >99.00% | |
An inhibitor of cyclin-dependent kinases | ||||
| GC39421 | PNU112455A hydrochloride | 21886-12-4 | >98.00% | |
PNU112455A hydrochloride是CDK2和CDK5的ATP位点的竞争性抑制剂，其对CDK2和CDK5中ATP位点的Km值分别为3.6μM和3.2μM。 | ||||
| GC39811 | FIT-039 | 1113044-49-7 | >98.00% | |
A Cdk9 inhibitor | ||||
| GC40092 | PD 0332991-d8 | 1628752-83-9 | >99.50% | |
An internal standard for the quantification of PD 0332991 | ||||
| GC41716 | (R)-CR8 | 294646-77-8 | >98.00% | |
An inhibitor of cyclin-dependent kinases | ||||
| GC43175 | CAY10574 | 140651-18-9 | >99.50% | |
A Cdk2-cyclin E and Cdk9 inhibitor | ||||
| GC45983 | Voruciclib | 1000023-04-0 | >99.50% | |
A pan-CDK inhibitor | ||||
| GC50217 | BS 181 dihydrochloride | 1883548-83-1 | - | |
BS 181 dihydrochloride 是一种比 Seliciclib 有效且选择性的 CDK7 抑制剂 (IC50\u003d21 nM)。 BS-181 还针对 CDK2、CDK5 和 CDK9，IC50 值分别为 880 nM、3000 nM 和 4200 nM（无法阻断 CDK1、4 和 6）。 BS 181 dihydrochloride 抑制一组癌细胞生长 (IC50\u003d11.5 μM-37.3 μM) 并诱导细胞凋亡。 BS 181 dihydrochloride 具有研究癌症治疗的潜力。 | ||||