GlpBio

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)

  • GC32735 structure
    GC32735Samuraciclib hydrochloride (ICEC0942 hydrochloride)
    CAS: 1805789-54-1
    纯度: >99.50%

    Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.

  • GC32741 structure
    GC32741CCT-251921
    CAS: 1607837-31-9
    纯度: >99.50%

    CCT-251921是有效，选择性，有口服活性的CDK8抑制剂；IC50值为2.3nM。

  • GC32746 structure
    GC32746MSC2530818
    CAS: 1883423-59-3
    纯度: >99.50%

    A Cdk8 inhibitor

  • GC32829 structure
    GC32829NU6300
    CAS: 2070015-09-5
    纯度: >96.00% / >98.00%

    NU6300是一种通过共价结合Gasdermin D (GSDMD)蛋白C191位点来特异性抑制细胞焦亡的小分子化合物。

  • GC32832 structure
    GC32832PF-06873600
    CAS: 2185857-97-8

    An inhibitor of Cdk2, Cdk4, and Cdk6

  • GC32845 structure
    GC32845PROTAC CDK9 Degrader-1
    CAS: 2118356-96-8
    纯度: >98.00%

    PROTACCDK9Degrader-1是一种有选择性的CDK9降解剂。

  • GC32898 structure
    GC32898SEL120-34A HCl
    CAS: 1609452-30-3

    A dual inhibitor of Cdk8 and Cdk19

  • GC32930 structure
    GC32930Simurosertib (TAK-931)
    CAS: 1330782-76-7
    纯度: >98.00%

    An inhibitor of Cdc7 kinase

  • GC32970 structure
    GC32970MBQ-167
    CAS: 2097938-73-1
    纯度: >98.00%

    MBQ-167是Ras相关的C3型肉毒素底物(Rac)和细胞分裂周期蛋白(Cdc42)的双抑制剂，其对Rac1/2/3的IC50值为103nM，对Cdc42的IC50值为78nM。

  • GC33049 structure
    GC33049FN-1501
    CAS: 1429515-59-2
    纯度: >98.00%

    FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.

  • GC33107 structure
    GC33107(±)-BAY-1251152
    CAS: 1610358-53-6
    纯度: >99.50%

    A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152

  • GC33137 structure
    GC33137SEL120-34A
    CAS: 1609522-33-9
    纯度: >99.50%

    A dual inhibitor of Cdk8 and Cdk19

  • GC33180 structure
    GC33180CDK8-IN-1
    CAS: 1629633-48-2

    CDK8-IN-1是一个有效的、CDK8的选择性抑制剂，其IC50值为3nM。

  • GC33327 structure
    GC33327CMPD 7
    CAS: 2220184-50-7
    纯度: >98.00%

    CMPD 7 是一种有效的选择性 CDK12 抑制剂，在酶促试验中的 IC50 为 491 nM。

  • GC33353 structure
    GC33353ON-013100
    CAS: 865783-95-5
    纯度: >98.00%

    ON-013100，一种抗肿瘤药物，作为有丝分裂的抑制剂，能够抑制细胞周期蛋白D1(CyclinD1)的表达。

  • GC33360 structure
    GC33360Roniciclib (BAY 1000394)
    CAS: 1223498-69-8
    纯度: >98.50%

    Roniciclib (BAY 1000394) 是一种可口服的泛细胞周期蛋白依赖性激酶 (CDK) 抑制剂，对 CDK1、CDK2、CDK3、CDK4、CDK7 和 CDK9 的 IC50 为 5-25 nM。

  • GC33366 structure
    GC33366CDK8-IN-4
    CAS: 1613638-82-6

    CDK8-IN-4是CDK8的抑制剂，来自专利WO2014090692A1,化合物实例16,IC50值为0.2nM。

  • GC34056 structure
    GC34056NVP-2
    CAS: 1263373-43-8
    纯度: >99.00%

    A Cdk9/cyclin T1 complex inhibitor

  • GC34059 structure
    GC34059Atuveciclib Racemate (BAY-1143572 Racemate)
    CAS: 1414943-88-6
    纯度: >98.00%

    Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.

  • GC34087 structure
    GC34087Trilaciclib hydrochloride (G1T28 hydrochloride)
    CAS: 1977495-97-8
    纯度: >98.00%

    Trilaciclib hydrochloride (G1T28 hydrochloride) (G1T28 hydrochloride) 是一种 CDK4/6 抑制剂，对 CDK4 和 CDK6 的 IC50 分别为 1 nM 和 4 nM。

  • GC34100 structure
    GC34100Lerociclib dihydrochloride (G1T38 dihydrochloride)
    CAS: 2097938-59-3
    纯度: >99.50%

    Lerociclib dihydrochloride (G1T38 dihydrochloride) (G1T38 dihydrochloride) 是一种有效的选择性 CDK4/CDK6 抑制剂，对 CDK4/CyclinD1 和 CDK6/CyclinD3 的 IC50 分别为 1 nM 和 2 nM。

  • GC34118 structure
    GC34118Trilaciclib (G1T28)
    CAS: 1374743-00-6

    Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively.

  • GC34124 structure
    GC34124(rel)-MC180295
    CAS: 2237942-08-2
    纯度: >98.00%

    MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.

  • GC34163 structure
    GC34163Lerociclib (G1T38)
    CAS: 1628256-23-4

    G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.