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)

  • GC10840 structure
    GC10840THZ1
    CAS: 1604810-83-4
    纯度: >98.50%

    A covalent Cdk7 inhibitor

  • GC10842 structure
    GC10842LEE011
    CAS: 1211441-98-3
    纯度: >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 structure
    GC11022SB 218078
    CAS: 135897-06-2
    纯度: >98.00%

    A potent Chk1 inhibitor

  • GC11040 structure
    GC11040Borrelidin
    CAS: 7184-60-3
    纯度: >98.00%

    An antiangiogenic antibiotic

  • GC11324 structure
    GC11324PHA-767491
    CAS: 845714-00-3

    A potent Cdc7 kinase inhibitor

  • GC11396 structure
    GC11396SNS-032 (BMS-387032)
    CAS: 345627-80-7
    纯度: >99.00%

    A Cdk2, Cdk7, and Cdk9 inhibitor

  • GC11401 structure
    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。

  • GC11774 structure
    GC11774KH CB19
    CAS: 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 structure
    GC11823LY2835219 free base
    CAS: 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。

  • GC11971 structure
    GC11971LY2857785
    CAS: 1619903-54-6
    纯度: >98.50%

    A Cdk9 inhibitor

  • GC12001 structure
    GC12001BS-181
    CAS: 1092443-52-1

    A selective Cdk7 inhibitor

  • GC12011 structure
    GC12011P276-00
    CAS: 920113-03-7
    纯度: >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 structure
    GC12064SB1317
    CAS: 937270-47-8
    纯度: >99.50%

    A multi-kinase inhibitor

  • GC12348 structure
    GC12348Ro 3306
    CAS: 872573-93-8
    纯度: >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 structure
    GC12425CDK inhibitor II
    CAS: 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。

  • GC12438 structure
    GC12438AZD-5438
    CAS: 602306-29-6
    纯度: >99.50%

    A potent inhibitor of CDKs

  • GC12612 structure
    GC12612JNJ-7706621
    CAS: 443797-96-4
    纯度: >99.50%

    A dual inhibitor of CDKs and Aurora kinases

  • GC12642 structure
    GC12642THZ1 Hydrochloride
    CAS: 1604810-83-4
    纯度: >98.00%

    A covalent Cdk7 inhibitor

  • GC12865 structure
    GC12865BMS265246
    CAS: 582315-72-8
    纯度: >99.00%

    A cell-permeable inhibitor of Cdk1 and Cdk2

  • GC12871 structure
    GC12871CDK9 inhibitor
    CAS: 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。

  • GC13328 structure
    GC13328XL413 hydrochloride
    CAS: 2062200-97-7
    纯度: >99.50%

    A potent inhibitor of Cdc7

  • GC13511 structure
    GC13511THZ2
    CAS: 1604810-84-5
    纯度: >99.50%

    A Cdk7 inhibitor

  • GC13690 structure
    GC13690BS-181 HCl
    CAS: 1397219-81-6
    纯度: >99.00%

    A selective Cdk7 inhibitor

  • GC13998 structure
    GC13998AT7519 Hydrochloride
    CAS: 902135-91-5
    纯度: >99.00%

    A Cdk inhibitor