1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. CDK

CDK

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 Isoform Specific Products:

  • CDK1

  • CDK2

  • CDK3

  • CDK4

  • CDK5

  • CDK6

  • CDK7

  • CDK8

  • CDK9

  • CDK11

  • CDK12

  • CDK13

  • CDK14

  • CDK16

  • CDK19

  • CDC

  • CLK

CDK 相关产品 (144):

Cat. No. Product Name Effect Purity
  • HY-50767
    Palbociclib Inhibitor 99.96%
    Palbociclib (PD 0332991) 是选择性的 CDK4CDK6 抑制剂,IC50 分别为11 nM,16 nM。 Palbociclib是一种治疗ER阳性和HER2阴性乳腺癌的药物。
  • HY-16297
    Abemaciclib methanesulfonate Inhibitor 99.95%
    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) 是选择性的 CDK4/6 抑制剂,抑制 CDK4/CDK6 的 IC50 分别为 2 nM 和 10 nM。
  • HY-50767A
    Palbociclib hydrochloride Inhibitor 99.94%
    Palbociclib hydrochloride是高选择性的 CDK4/6 抑制剂,IC50 分别为11 nM 和 16 nM。
  • HY-15777
    Ribociclib Inhibitor 99.85%
    Ribociclib (LEE011) 是一种高度特异性的 CDK4/6 抑制剂,IC50 值分别为 10 nM 和 39 nM,对 cyclin B/CDK1 复合体的活性低于其 1000 倍。
  • HY-10492
    Dinaciclib Inhibitor 99.73%
    Dinaciclib 是一种有效的选择性 CDK 抑制剂,抑制 CDK2CDK5CDK1CDK9IC50 分别为 1,1,3 和 4 nM。
  • HY-117535
    CDK2-IN-4 Inhibitor
    CDK2-IN-4 是一种有效选择性的 CDK2 抑制剂,对 CDK2/cyclin A 的 IC50 值为 44 nM,选择性高出 CDK1/cyclin B 的 2,000 倍 (IC50=86 μM)。
  • HY-120350
    BI-1347 Inhibitor 99.83%
    BI-1347 是一种有效的 CDK8 抑制剂,IC50 值为 1.1 nM,详细信息请参考 WO2017202719A1 中的产物 I-003。
  • HY-128587
    SY-1365 Inhibitor
    SY-1365 是一种高选择性的 CDK7 共价抑制剂,具有治疗血液学疾病和实体肿瘤潜力。
  • HY-103618
    THZ531 Inhibitor 99.86%
    THZ531 是 CDK12CDK13 的共价抑制剂,其 IC50 值分别为 158 nM 和 69 nM。
  • HY-30237
    Seliciclib Inhibitor 99.94%
    Seliciclib (Roscovitine) 是一种口服有效的,选择性的 CDKs 抑制剂,抑制 CDK5CDK2CDK2IC50 分别为0.2 μM,0.65 μM,0.7 μM。
  • HY-80013
    THZ1 Inhibitor 98.82%
    THZ1 是有效,选择性的共价 CDK7 抑制剂,IC50 为 3.2 nM。THZ1 还抑制相关的激酶 CDK12CDK13,并下调 MYC 表达。
  • HY-10005
    Flavopiridol Inhibitor 99.72%
    Flavopiridol (Alvocidib; L868275; HMR-1275) 是一种竞争型的 CDK 广谱抑制剂, 抑制 CDK1,CDK2,CDK4的IC50 分别为30,170,100 nM。
  • HY-12529
    Ro-3306 Inhibitor
    Ro-3306 是一种有效,选择性的 CDK1 抑制剂,对 CDK1,CDK1/cyclin B1 和 CDK2/cyclin E 的 Ki 值为分别为 20 nM,35 nM 和 340 nM。
  • HY-12214A
    NVP-2 Inhibitor 99.29%
    NVP-2 是一种 CDK9 抑制剂,其 IC50 值为 0.5 nM。
  • HY-A0065
    Palbociclib isethionate Inhibitor 99.96%
    Palbociclib isethionate是高选择性的 CDK4/6 抑制剂,IC50 为11 nM/16 nM。
  • HY-16297A
    Abemaciclib Inhibitor 99.69%
    Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂,能够抑制 CDK4/CDK6 的活性,IC50 分别为 2 nM 和 10 nM。
  • HY-101212
    CYC065 Inhibitor 99.78%
    CYC065 是第二代口服有效的 ATP 竞争性的 CDK2 / CDK9 激酶抑制剂。
  • HY-112088
    AZD4573 Inhibitor 99.80%
    AZD4573 是一种有效且高度选择性的 CDK9 抑制剂 (IC50 值小于 4 nM),并能够短暂靶向治疗血液恶性肿瘤。
  • HY-80013A
    THZ1 Hydrochloride Inhibitor 98.70%
    THZ1 Hydrochloride 是有效,选择性的共价 CDK7 抑制剂,IC50 为 3.2 nM。THZ1 Hydrochloride 还抑制相关的激酶 CDK12CDK13,并下调 MYC 表达。
  • HY-114177
    PF-06873600 Inhibitor 99.98%
    PF-06873600 是具有口服活性的、细胞周期蛋白依赖性激酶 (CDK) 的选择性抑制剂,其对 CDK2、CDK4 和 CDK6 的 Ki 值分别为 0.09 nM、0.13 nM 和 0.16 nM. PF-06873600 具有潜在的抗肿瘤活性。
Isoform Specific Products

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