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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)

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

    CT7001 hydrochloride (ICEC0942 hydrochloride) (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. CT7001 hydrochloride (ICEC0942 hydrochloride) displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. CT7001 hydrochloride (ICEC0942 hydrochloride) inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. CT7001 hydrochloride (ICEC0942 hydrochloride) has anti-tumor effects.

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

    CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.

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

    A Cdk8 inhibitor

  • GC32829 structure
    GC32829NU6300
    CAS: 2070015-09-5
    Purity: >98.00%

    NU6300 is a small molecule compound that specifically inhibits pyroptosis by covalently binding to the C191 site of the Gasdermin D (GSDMD) protein.

  • GC32832 structure
    GC32832PF-06873600
    CAS: 2185857-97-8
    Purity: >98%
  • GC32845 structure
    GC32845PROTAC CDK9 Degrader-1
    CAS: 2118356-96-8
    Purity: >98.00%

    PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.

  • GC32898 structure
    GC32898SEL120-34A HCl
    CAS: 1609452-30-3
    Purity: >98%

    SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

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

    Simurosertib (TAK-931) (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib (TAK-931) has anti-cancer activity.

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

    MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC50s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.

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

    FN-1501 is a potent inhibitor of FLT3 and 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. FN-1501 has anticancer activity.

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

    (±)-BAY-1251152 ((±)-BAY-1251152) is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

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

    SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

  • GC33180 structure
    GC33180CDK8-IN-1
    CAS: 1629633-48-2
    Purity: >98%

    CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

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

    CMPD 7 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.

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

    ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.

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

    Roniciclib (BAY 1000394) is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.

  • GC33366 structure
    GC33366CDK8-IN-4
    CAS: 1613638-82-6
    Purity: >98%

    CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.

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

    NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 ?M, 0.706 ?M, and 0.605 ?M, respectively. NVP-2 induces cell apoptosis.

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

    Atuveciclib Racemate (BAY-1143572 Racemate) (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

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

    Trilaciclib hydrochloride (G1T28 hydrochloride) (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

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

    Lerociclib dihydrochloride (G1T38 dihydrochloride) (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

  • GC34118 structure
    GC34118Trilaciclib (G1T28)
    CAS: 1374743-00-6
    Purity: >98%

    Trilaciclib (G1T28) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

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

    (rel)-MC180295 ((rel)-(rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. (rel)-MC180295 also inhibits GSK-3α and GSK-3β. (rel)-MC180295 ((rel)-(rel)-MC180295) has potent anti-tumor effect.

  • GC34163 structure
    GC34163Lerociclib (G1T38)
    CAS: 1628256-23-4
    Purity: >98%

    Lerociclib (G1T38) (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.