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

CDK

Cyclin dependent kinase

CDK

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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 Isoform Specific Products:

CDK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-177743
    TR-213
    		Degrader
    TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer.
    TR-213
  • HY-111244
    DCB-3503
    		Inhibitor
    DCB-3503 is an allosteric modulator of heat shock cognate protein HSC70 and an inhibitor of Cyclin D1. DCB-3503 inhibits Cyclin D1 translation by allosterically modulating the ATPase and chaperone activities of HSC70. DCB-3503 may inhibit malignancies such as hepatocellular carcinoma or breast cancer with elevated expression of cyclin D1.
    DCB-3503
  • HY-E70685
    CDK5/p35NCK Recombinant Human Active Protein Kinase
    CDK5 can be mapped to chromosome 7q36 and its expression is upregulated by the transcription factors Fos and CREB through the MEK/ERK pathway and by δFosB. CDK5 plays a vital role in the central nervous system but has functions in other cell types. CDK5 has recently been implicated in diseases, including the development and progression of cancer and neurodegenerative diseases. CDK5/p35NCK Recombinant Human Active Protein Kinase is an ortholog of CDK5.
    CDK5/p35NCK Recombinant Human Active Protein Kinase
  • HY-133956
    3-ATA
    		Inhibitor
    3-ATA (NSC 680434) is a selective inhibitor of cyclin-dependent kinase 4 (CDK4) with neuroprotective and antitumor effects. 3-ATA can alleviate kainic acid (HY-N2309)-induced apoptosis in cerebellar granule neurons, which can be used in the study of neurodegenerative diseases.
    3-ATA
  • HY-110359
    CGP-74514 dihydrochloride
    		Inhibitor
    CGP-74514 dihydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 dihydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 dihydrochloride is promising for research of bladder cancer.
    CGP-74514 dihydrochloride
  • HY-E70661
    CDK14/CycY Recombinant Human Active Protein Kinase
    CDK14 is a member of the TAIRE subfamily. CDK14/CycY Recombinant Human Active Protein Kinase is an ortholog of CDK14. CDK14/CycY phosphorylates S1490 of LRP6 during the G2/M transition in a Wnt-independent manner.
    CDK14/CycY Recombinant Human Active Protein Kinase
  • HY-162293
    CDK8-IN-14
    		Inhibitor
    CDK8-IN-14 (compound 12) inhibits CDK8 with an IC50 value of 39.2 nM and has anti-AML cell proliferation activity (molm-13 GC50 = 0.02±0.01μM, MV4-11 GC50 = 0.03±0.01μM).
    CDK8-IN-14
  • HY-181004
    PKMYT1-IN-13
    		Inhibitor
    PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer.
    PKMYT1-IN-13
  • 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 can be used for the study of leukemia, gastric and ovarian carcinoma.
    SST0116CL1
  • HY-157980
    CDK9-IN-32
    		Inhibitor
    CDK9-IN-32 (compound 006-3) is a CDK9 inhibitor.
    CDK9-IN-32
  • HY-181565A
    CDK7-IN-33 maleate
    		Inhibitor
    CDK7-IN-33 maleate is an orally active pyrimidine derivative and also a CDK7 kinase inhibitor. CDK7-IN-33 maleate is applicable to the research of cancer, inflammation, cardiovascular diseases, infectious diseases, immune diseases and metabolic diseases.
    CDK7-IN-33 maleate
  • HY-108136
    Bisindolylmaleimide X
    		Antagonist
    Bisindolylmaleimide X (Ro 31-8425, BIM-X) is a cell-penetrating PKC inhibitor. Bisindolylmaleimide X is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM. Bisindolylmaleimide X inhibits the proliferation of CD4 T cells in vitro. Bisindolylmaleimide X inhibits eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. Bisindolylmaleimide X can be used for research on the immune system and cardiovascular diseases.
    Bisindolylmaleimide X
  • 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-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-181769
    Anticancer agent 306
    		Inhibitor
    Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer.
    Anticancer agent 306
  • HY-P11013
    p27
    		Inhibitor
    p27, a CDK inhibitor, is a SCFSkp2/Cks1 substrate. p27 can be used for the study of cancer.
    p27
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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