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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)

  • GC78957 structure
    GC78957(2S,3R,4S)-ASX-173
    CAS: 2748800-07-7
    Purity: >99.00%

    (2S,3R,4S)-ASX-173 is the (2S,3R,4S)-enantiomer of ASX-173.

  • GC78958 structure
    GC78958TMLB-C16
    CAS: 2923531-50-2
    Purity: >99.00%

    TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a K D of 3.962 μM.

  • GC78998 structure
    GC78998CTX-439
    CAS: 2377487-13-1
    Purity: >98%

    CTX-439 is an orally active, ATP-competitive small-molecule inhibitor of CDK12 and CDK13, with an IC 50 of 3.1 nM and a K d of 0.38 nM against CDK12, and an IC 50 of 9.2 nM against CDK13.

  • GC78999 structure
    GC78999CID-078
    CAS: 3064485-16-8
    Purity: >99.00%

    CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor.

  • GC79000 structure
    GC79000Q901 TFA
    Purity: >98.50%

    Q901 (CDK7-IN-21) TFA is a selective and potent CDK7 inhibitor with an IC 50 of 10 nM.

  • GC79006 structure
    GC79006CDK2 degrader 8
    CAS: 3099145-52-2
    Purity: >98%

    CDK2 degrader 8 is a selective cyclin-dependent kinase 2 ( CDK2 ) degrader.

  • GC79007 structure
    GC79007Cdk2/Cyclin Inhibitory Peptide I acetate
    Purity: >99.50%

    Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) acetate, a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner [1] .

  • GC79077 structure
    GC79077DDO-6600
    CAS: 2640292-37-9
    Purity: >98.00%

    DDO-6600 is a covalent Hsp90 inhibitor.

  • GC79108 structure
    GC79108AP4-43
    Purity: >99.50%

    AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor.

  • GC79121 structure
    GC79121XL495
    CAS: 3040320-93-9
    Purity: >98%

    XL495 is an potent, selective and orally active PKMYT1 inhibitor.

  • GC79176 structure
    GC79176ARUK2010489
    Purity: >96.50%

    ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC 50 of 8.7.

  • GC80882 structure
    GC80882ZLY025
    CAS: 3070379-34-6
    Purity: >99.00%

    ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC 50 of 42.7 nM.

  • GC80884 structure
    GC80884CXJ2080
    Purity: >98%

    CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC 50 of 0.88 nM.

  • GC80885 structure
    GC80885PROTAC CDK6 Degrader 1
    Purity: >98.50%

    PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC 50 of 0.037 μM.

  • GC80886 structure
    GC80886PROTAC CDK2/4/6 Degrader-2
    CAS: 2541626-49-5
    Purity: >97.00%

    PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader.

  • GC80892 structure
    GC80892SR-5037
    CAS: 2387704-74-5
    Purity: >99.50%

    SR-5037 is an orally active CDK12 ( IC 50 = 31 nM)/ CDK13 inhibitor and CycK ( DC 50 = 30 nM; D max > 98%) molecular glue degrader.

  • GC80893 structure
    GC80893PROTAC CDK2/4 Degrader-1
    Purity: >98.00%

    PROTAC CDK2/4 Degrader-1 is a PROTAC degrader of cyclin-dependent kinase 2 ( CDK2 ) and cyclin-dependent kinase 4 ( CDK4 ).

  • GC80894 structure
    GC80894(S)-JWZ-5-13
    Purity: >99.50%

    (S)-JWZ-5-13 (compound 17-Neg), a PROTAC CDK7 degrader, is a negative control compound of JWZ-5-13.

  • GC80896 structure
    GC80896PROTAC D16-M1P2
    Purity: >98%

    PROTAC D16-M1P2 is an orally active CRBN -mediated selective PKMYT1 PROTAC degrader, with a DC 50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells.

  • GC81307 structure
    GC81307DYRK2-IN-2
    CAS: 2416195-65-6
    Purity: >98%

    DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC 50 value being 40.3 nM.

  • GC81308 structure
    GC81308DYRK2-IN-2 hydrochloride
    Purity: >98.00%

    DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC 50 of 40.3 nM.

  • GC81309 structure
    GC81309AO-365/43472821
    CAS: 1081122-55-5
    Purity: >99.50%

    AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A ( DYRK1A ) inhibitor ( IC 50 = 0.29 μM) and shows a significant inhibitory effect on ( CDC-like kinase 1) CLK1 ( IC 50 = 0.08 μM).

  • GC81336 structure
    GC81336KY19334
    CAS: 2319609-67-9
    Purity: >99.50%

    KY19334 is a CXXC5-DVL inhibitor.

  • GC81394 structure
    GC81394PPA-037 TFA
    Purity: >99.00%

    PPA-037 TFA is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 ( CDK12 ).