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

CDK

Cyclin dependent kinase

CDK

Related Products

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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-112842
    MBQ-167
    		Inhibitor 99.64%
    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.
    MBQ-167
  • HY-120350
    BI-1347
    		Inhibitor 99.84%
    BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.
    BI-1347
  • HY-137478A
    KB-0742 dihydrochloride
    		Inhibitor 99.24%
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
    KB-0742 dihydrochloride
  • HY-15338
    TG003
    		Inhibitor 99.57%
    TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
    TG003
  • HY-103019
    (+)-Enitociclib
    		Inhibitor 99.89%
    (+)-Enitociclib ((+)-BAY-1251152) is the enantiomer of Enitociclib (HY-103019E) with (+) optical rotation. Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.
    (+)-Enitociclib
  • HY-10012
    AZD-5438
    		Inhibitor 99.91%
    AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .
    AZD-5438
  • HY-123937
    THAL-SNS-032
    		Inhibitor 99.16%
    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
    THAL-SNS-032
  • HY-126675A
    AS2863619
    		Inhibitor 99.94%
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
    AS2863619
  • HY-W050154
    Kojic acid
    		Inhibitor 99.99%
    Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity.
    Kojic acid
  • HY-10006
    Flavopiridol Hydrochloride
    		Inhibitor 99.73%
    Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
    Flavopiridol Hydrochloride
  • HY-15777A
    Ribociclib hydrochloride
    		Inhibitor 99.95%
    Ribociclib hydrochloride (LEE011 hydrochloride) 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.
    Ribociclib hydrochloride
  • HY-139039
    BSJ-4-116
    		Inhibitor 98.73%
    BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).
    BSJ-4-116
  • HY-101257
    YKL-5-124
    		Inhibitor 98.79%
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
    YKL-5-124
  • HY-15777B
    Ribociclib succinate
    		Inhibitor 99.93%
    Ribociclib succinate (LEE011 succinate) 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.
    Ribociclib succinate
  • HY-101212
    Fadraciclib
    		Inhibitor 99.78%
    Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.
    Fadraciclib
  • HY-115470
    CLK-IN-T3
    		Inhibitor 98.63%
    CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
    CLK-IN-T3
  • HY-18340
    (R)​-​CR8
    		Inhibitor 99.61%
    (R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
    (R)​-​CR8
  • HY-15339
    CVT-313
    		Inhibitor 99.90%
    CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
    CVT-313
  • HY-101467
    Trilaciclib
    		Inhibitor 99.32%
    Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy.
    Trilaciclib
  • HY-132868
    SLK/STK10-IN-1
    		Inhibitor 99.78%
    SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.
    SLK/STK10-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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