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)

  • GC73224 structure
    GC73224CLK1-IN-3
    CAS: 2922550-28-3
    纯度: >98.00%

    CLK1-IN-3(化合物10ad)是一种有效的选择性Clk1抑制剂,IC50为5 nM,对Dyrk1A的选择性超过300倍。

  • GC73264 structure
    GC73264Multi-target kinase inhibitor 2
    纯度: >99.00%

    Multi-target kinase inhibitor 2(化合物5K)是一种多靶点激酶抑制剂,对EGFR、Her2、VEGFR2和CDK2酶具有活性,IC50值在40至204 nM之间。

  • GC73270 structure
    GC73270XPW1
    CAS: 2700286-66-2
    纯度: >99.00%

    XPW1是一种强效、选择性CDK9抑制剂,对透明细胞肾细胞癌(ccRCC)具有优异的活性和低毒性。

  • GC73286 structure
    GC73286PROTAC CDK9 degrader-7
    CAS: 2935587-90-7
    纯度: >99.00%

    PROTAC CDK9 degrader-7是一种特异性靶向CDK9的PROTAC。

  • GC73288 structure
    GC73288CDK8-IN-13
    CAS: 918523-75-8
    纯度: >98.00%

    CDK8-IN-13是一种强效、选择性且口服有效的CDK8抑制剂,IC 50 值为51.9nM。

  • GC73345 structure
    GC73345CDK8-IN-11
    CAS: 2839338-28-0
    纯度: >98.00%

    CDK8-IN-11是一种有效的选择性CDK8抑制剂,IC50值为46 nM。

  • GC73426 structure
    GC73426MFH290
    CAS: 2088715-91-5
    纯度: >98.00%

    MFH290是一种有效的高选择性细胞周期蛋白依赖性激酶12/13 (CDK12/13)共价抑制剂。

  • GC73429 structure
    GC73429CDK7-IN-21
    CAS: 2766124-39-2
    纯度: >96.00%

    CDK7-IN-21(化合物A22)是一种有效的CDK7抑制剂。

  • GC73504 structure
    GC73504SRX3177
    CAS: 2241237-51-2
    纯度: >99.00%

    SRX3177是CDK4/6、PI3K和BRD4的三重抑制剂,IC50分别为33 nM(BRD4 BD1)、89 nM(BR D4 BD2)、79 nM(PI3Kα)、83 nM(PI 3Kδ)、3.18μM(PI3Kγ)、<2.5 nM(CDK4)、3.3 nM(CDK6)。

  • GC73590 structure
    GC73590MAPK-IN-2
    纯度: >98.00%

    MAPK-IN-2(化合物3h)是一种具有抗肿瘤活性的强效MAPK抑制剂。

  • GC73597 structure
    GC73597ZNL-05-044
    纯度: >99.00%

    ZNL-05-044是一种CDK11抑制剂,对CDK11A和CDK11B的ic50分别为0.23 μM和0.27 μM (NanoBRET测定)。

  • GC73758 structure
    GC73758Ribociclib-d8
    CAS: 2167898-24-8
    纯度: >99.00%

    Ribociclib-d8是氘标记的Ribociclib。

  • GC73787 structure
    GC73787AZD8421
    CAS: 3047321-53-6
    纯度: >98.00%

    AZD8421是一种对CDK1、CDK4和CDK6具有选择性的CDK2抑制剂(IC50:9 nM)。

  • GC73880 structure
    GC73880DS17
    纯度: >98.00%

    DS17是一种分子胶,作为cyclin K的有效降解剂,EC50为13 nM。

  • GC73893 structure
    GC73893BLU-222
    CAS: 2888704-84-3
    纯度: >98.00%

    BLU-222是一种口服活性高选择性CDK2抑制剂。

  • GC73934 structure
    GC73934Cyclin K degrader 1
    纯度: >99.00%

    Cyclin K degrader 1(化合物40)是一种基于AT7519的Cyclin K降解剂,DC50为21 nM。

  • GC73965 structure
    GC73965INX-315
    CAS: 2745060-92-6
    纯度: >99.00%

    INX-315是一种口服活性和选择性CDK2抑制剂,可诱导细胞周期阻滞在G1期。

  • GC73970 structure
    GC73970CDDD11-8
    CAS: 2241659-94-7
    纯度: >99.00%

    CDDD11-8是CDK9和FLT3-ITD的口服活性、强效和选择性抑制剂,Ki值分别为8和13 nM。

  • GC73976 structure
    GC73976CDK2-IN-23
    CAS: 2488073-20-5
    纯度: >99.00%

    CDK2-IN-23(化合物17)是激酶选择性和高效CDK2抑制剂(IC50=0.29nM)。

  • GC74050 structure
    GC74050PROTAC CDK4/6 degrader 1
    CAS: 3025082-14-5
    纯度: >98.00%

    PROTAC CDK4/6 degrader 1(化合物7f)是CDK4和CDK6的双重降解剂,DC50分别为10.5和2.5 nM。

  • GC74161 structure
    GC74161Palbociclib hydrochloride
    CAS: 571189-11-2
    纯度: >99.50%

    Palbociclib hydrochloride (PD 0332991)是一种口服选择性CDK4和CDK6抑制剂,IC50值分别为11 nM和16 nM。

  • GC74261 structure
    GC74261(R)-(+)-O-Demethylbuchenavianine
    CAS: 1364123-68-1
    纯度: >98.00%

    (R)-(+)-O-Demethylbuchenavianine是细胞周期蛋白依赖性激酶CDK的抑制剂。

  • GC74262 structure
    GC74262(S)-(-)-O-Demethylbuchenavianine
    CAS: 91147-18-1
    纯度: 不显示

    (S)-(-)-O-Demethylbuchenavianine(化合物(S)-(−)-1)是一种黄酮类生物碱。

  • GC74324 structure
    GC74324Cdk5i peptide
    CAS: 2298317-00-5
    纯度: >99.00%

    Cdk5i peptide是一个由Cdk5衍生的12个氨基酸的肽片段。