1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. CDK

CDK

Cyclin dependent kinase

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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-164399
    SST0116CL1
    Degrader
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth.
    SST0116CL1
  • HY-157980
    CDK9-IN-32
    Inhibitor
    CDK9-IN-32 (compound 006-3) is a CDK9 inhibitor.
    CDK9-IN-32
  • HY-143258
    CDK4/6-IN-8
    Inhibitor
    CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC50 values of 5.01 nM and 3.97 nM, respectively.
    CDK4/6-IN-8
  • HY-156296
    CDK9-Cyclin T1 PPI-IN-1
    Inhibitor
    CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model.
    CDK9-Cyclin T1 PPI-IN-1
  • HY-171786
    CDK12-IN-8
    Inhibitor
    CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer.
    CDK12-IN-8
  • HY-111931
    Indirubin-3'-monoxime-5-sulphonic acid
    Inhibitor
    Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.
    Indirubin-3'-monoxime-5-sulphonic acid
  • HY-E70663
    CDK15/CycB1 Recombinant Human Active Protein Kinase
    CDK15 is a cell cycle-dependent kinase that is involved in tumor progression. CDK15/CycB1 Recombinant Human Active Protein Kinase is an ortholog of CDK15.
    CDK15/CycB1 Recombinant Human Active Protein Kinase
  • HY-123668
    KM05382
    Inhibitor
    KM05382 serves as an inhibitor of CDK9 and reduces the transcription of GAPDH.
    KM05382
  • HY-150213
    ODN BW001
    Inhibitor
    ODN BW001 is an oligodeoxynucleotide (ODN). ODN BW001 plays a regulatory role in the proliferation and activation of osteoblast.
    ODN BW001
  • HY-P11013
    p27
    Inhibitor
    p27, a CDK inhibitor, is a SCFSkp2/Cks1 substrate. p27 can be used for the study of cancer.
    p27
  • HY-E70659
    CDK12/CycK Recombinant Human Active Protein Kinase
    CDK12/CycK Recombinant Human Active Protein Kinase is a cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of RNA polymerase II (Pol II), thereby regulating different phases of the transcription cycle from transcription initiation to elongation and termination.
    CDK12/CycK Recombinant Human Active Protein Kinase
  • HY-E70668
    CDK19/CycC Recombinant Human Active Protein Kinase
    CDK19 is a kinase that controls the dynamic transcription of specific genes in response to various signals. CDK19 is hijacked by various solid and liquid tumors to maintain excessive cell proliferation. CDK19/CycC Recombinant Human Active Protein Kinase is an ortholog of CDK19.
    CDK19/CycC Recombinant Human Active Protein Kinase
  • HY-156470
    Multi-kinase-IN-6
    Inhibitor
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
  • HY-161379
    CLZX-205
    Inhibitor
    CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC50 of 2.9 nM. CLZX-205 plays an important role in cancer research.
    CLZX-205
  • HY-153426
    CDK9-IN-23
    Inhibitor
    CDK9-IN-23 (Example 4) is a CDK9 inhibitor with an IC50 of <20 nM.
    CDK9-IN-23
  • HY-145867
    EGFR-IN-45
    Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-150641
    CDK-IN-9
    Inhibitor
    CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
    CDK-IN-9
  • HY-18969
    LDC3140
    Inhibitor
    LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment.
    LDC3140
  • HY-178452
    PROTAC CDK4/6/9 degrader 1
    Degrader
    PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)).
    PROTAC CDK4/6/9 degrader 1
  • HY-112336
    Aloisine RP106
    Inhibitor
    Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively.
    Aloisine RP106
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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