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)

  • GC74727 structure
    GC74727JSH-009
    CAS: 2247481-08-7
    纯度: 不显示

    JSH-009是一种新型的高选择性CDK9抑制剂,对调节转录伸长至关重要。

  • GC91419 structure
    GC91419CYY292
    CAS: 2644673-04-9
    纯度: >98.00%

    CYY292是一种PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂,它们的IC50分别为5.35、4.6、28、28和78 nM。

  • GN10017 structure
    GN10017Wogonin
    CAS: 632-85-9
    纯度: >99.50%

    A flavonoid with anti-inflammatory and antitumor activities

  • GN10526 structure
    GN10526Cucurbitacin E
    CAS: 18444-66-1
    纯度: >99.50%

    A natural triterpene

  • GN10696 structure
    GN10696Garcinone C
    CAS: 76996-27-5

    Garcinone C 是一种黄酮衍生物,是一种从 Garcinia oblongifolia Champ 中提取的天然化合物,用作抗炎、收敛和促进肉芽的药物,对某些癌症具有潜在的细胞毒性作用。 Garcinone C 刺激 ATR 和 4E-BP1 的表达水平,同时有效抑制 cyclin B1、cyclin D1、cyclin E2、cdc2、Stat3 和 CDK7 的表达水平。 Garcinone C 以时间和剂量依赖性方式显着抑制人鼻咽癌 (NPC) 细胞系 CNE1、CNE2、HK1 和 HONE1 的细胞活力。