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CDK

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<div class="colum_1 clearer"><p>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.</p><p>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.</p><p>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 <i>S. pombe</i> (Cdc2), <i>S. cerevisia</i> (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).</p></div>

Products Related to CDK(299)

  • GC37522 structure
    GC37522RGB-286638
    CAS: 784210-87-3
    Purity: >99.50%

    A multi-kinase inhibitor

  • GC37523 structure
    GC37523RGB-286638 free base
    CAS: 784210-88-4
    Purity: >98%

    A multi-kinase inhibitor

  • GC37529 structure
    GC37529Ribociclib succinate hydrate
    CAS: 1374639-79-8
    Purity: >99.50%

    Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

  • GC37627 structure
    GC37627Senexin A
    CAS: 1366002-50-7
    Purity: >99.50%

    Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.

  • GC37709 structure
    GC37709SY-1365
    CAS: 1816989-16-8
    Purity: >99.00%

    SY-1365 (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. SY-1365 exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. SY-1365 possesses anti-tumor activity in hematological and multiple aggressive solid tumors.

  • GC37786 structure
    GC37786THZ1-R
    CAS: 1621523-07-6
    Purity: >98.00%

    A non-cysteine reactive derivative of THZ1

  • GC38330 structure
    GC38330EHT 5372
    CAS: 1425945-60-3
    Purity: >98%
  • GC38377 structure
    GC38377(2S,3R)-Voruciclib hydrochloride
    Purity: >98.00%

    (2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. (2S,3R)-Voruciclib is an orally active CDK inhibitor.

  • GC38482 structure
    GC38482Desmethylglycitein
    CAS: 17817-31-1
    Purity: >98%

    Desmethylglycitein, a metabolite of daidzein, is a potent tyrosinase inhibitor with an IC 50 value of 9.2μM for mushroom tyrosinase.

  • GC38736 structure
    GC38736AS2863619
    CAS: 2241300-51-4
    Purity: >98.00%

    AS2863619 is an orally administered small molecule inhibitor of cyclin-dependent kinase (CDK) 8 and 19 with IC 50 of 0.6099nM and 4.277nM, respectively.

  • GC38737 structure
    GC38737AS2863619 free base
    CAS: 2241300-50-3
    Purity: >99.50%

    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases.

  • GC38749 structure
    GC38749Abemaciclib metabolite M20
    CAS: 2138499-06-4
    Purity: >98.00%

    Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.

  • GC38755 structure
    GC38755CKI-7
    CAS: 120615-25-0
    Purity: >99.00%

    CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

  • GC38899 structure
    GC38899CDK ligand for PROTAC hydrochloride
    Purity: >98%
  • GC39162 structure
    GC39162TCMDC-135051
    CAS: 2413716-15-9
    Purity: >98%

    TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity.

  • GC39175 structure
    GC39175SR-4835
    CAS: 2387704-62-1
    Purity: >99.50%

    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.

  • GC39281 structure
    GC39281(R)-CR8 trihydrochloride
    CAS: 1786438-30-9
    Purity: >99.00%

    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor.

  • GC39421 structure
    GC39421PNU112455A hydrochloride
    CAS: 21886-12-4
    Purity: >98.00%

    PNU112455A hydrochloride is a competitive inhibitor of the ATP sites of CDK2 and CDK5, with the Km values for the ATP sites of CDK2 and CDK5 being 3.6 and 3.2μM, respectively.

  • GC39811 structure
    GC39811FIT-039
    CAS: 1113044-49-7
    Purity: >98.00%

    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1.

  • GC40092 structure
    GC40092PD 0332991-d8
    CAS: 1628752-83-9
    Purity: >99.50%

    Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.

  • GC41716 structure
    GC41716(R)-CR8
    CAS: 294646-77-8
    Purity: >98.00%

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy.

  • GC43175 structure
    GC43175CAY10574
    CAS: 140651-18-9
    Purity: >99.50%

    CAY10574 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAY10574 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

  • GC45983 structure
    GC45983Voruciclib
    CAS: 1000023-04-0
    Purity: >99.50%

    A pan-CDK inhibitor

  • GC50217 structure
    GC50217BS 181 dihydrochloride
    CAS: 1883548-83-1
    Purity: >98%

    Selective cdk7 inhibitor