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)

  • GC14162 structure
    GC14162ML167
    CAS: 1285702-20-6
    纯度: >98.50%

    A selective Clk4 inhibitor

  • GC14182 structure
    GC14182Kenpaullone
    CAS: 142273-20-9
    纯度: >98.00%

    A inhibitor of cyclin-dependent kinase and GSK3β

  • GC14230 structure
    GC14230K03861
    CAS: 853299-07-7
    纯度: >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 structure
    GC14707Purvalanol A
    CAS: 212844-53-6
    纯度: >99.00%

    A selective inhibitor of cyclin-dependent kinases

  • GC14974 structure
    GC14974AMG 925
    CAS: 1401033-86-0
    纯度: >98.00%

    A dual inhibitor of FLT3 and Cdk4

  • GC14987 structure
    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。

  • GC15047 structure
    GC15047PHA-793887
    CAS: 718630-59-2
    纯度: >98.00%

    A CDK inhibitor

  • GC15377 structure
    GC15377LEE011 succinate
    CAS: 1374639-75-4
    纯度: >99.50%

    A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor

  • GC15421 structure
    GC15421Palbociclib (PD0332991) Isethionate
    CAS: 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。

  • GC15571 structure
    GC15571SU 9516
    CAS: 377090-84-1
    纯度: >99.50%

    A pro-apoptotic Cdk2/cyclin A inhibitor

  • GC15588 structure
    GC15588PHA-848125
    CAS: 802539-81-7
    纯度: >99.50%

    An inhibitor of Cdks

  • GC15597 structure
    GC15597AT7519 trifluoroacetate
    CAS: 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。

  • GC15607 structure
    GC15607ON123300
    CAS: 1357470-29-1
    纯度: >99.00%

    A multi-kinase inhibitor

  • GC15841 structure
    GC15841Alsterpaullone
    CAS: 237430-03-4
    纯度: >98.00%

    A dual CDK and GSK3 inhibitor

  • GC15870 structure
    GC15870AT7519
    CAS: 844442-38-2
    纯度: >99.50%

    A Cdk inhibitor

  • GC15922 structure
    GC15922LEE011 hydrochloride
    CAS: 1211443-80-9
    纯度: >98.00%

    A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor

  • GC16063 structure
    GC16063Flavopiridol
    CAS: 146426-40-6
    纯度: >98.00%

    An inhibitor of cyclin-dependent kinases

  • GC16268 structure
    GC16268Purvalanol B
    CAS: 212844-54-7
    纯度: >98.50%

    A CDK inhibitor

  • GC16420 structure
    GC16420THZ531
    CAS: 1702809-17-3
    纯度: >98.00%

    An inhibitor of Cdk12 and Cdk13

  • GC16425 structure
    GC16425Flavopiridol hydrochloride
    CAS: 131740-09-5
    纯度: >98.00%

    An inhibitor of cyclin-dependent kinases

  • GC16511 structure
    GC16511OTS964
    CAS: 1338545-07-5
    纯度: >99.00%

    A TOPK inhibitor

  • GC16822 structure
    GC16822LY2835219
    CAS: 1231930-82-7
    纯度: >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 structure
    GC16959NVP-LCQ195
    CAS: 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。

  • GC17067 structure
    GC17067LDC000067
    CAS: 1073485-20-7
    纯度: >98.50%

    A Cdk9 inhibitor