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-145599A
    Tanuxiciclib trihydrochloride
    		Inhibitor ≥98.0%
    Tanuxiciclib trihydrochloride is a cyclin dependent kinase (CDK) inhibitor.
    Tanuxiciclib trihydrochloride
  • HY-143497
    HDAC1/2 and CDK2-IN-1
    		Inhibitor
    HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.
    HDAC1/2 and CDK2-IN-1
  • HY-16559A
    Riviciclib
    		Inhibitor
    Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.
    Riviciclib
  • HY-130515
    Cdc7-IN-3
    		Inhibitor
    Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
    Cdc7-IN-3
  • HY-131063
    CDK6/9-IN-1
    		Inhibitor
    CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.
    CDK6/9-IN-1
  • HY-156646
    Tibremciclib
    		Inhibitor
    Tibremciclib is a CDK4 inhibitor with antineoplastic activity.
    Tibremciclib
  • HY-15681A
    Senexin A hydrochloride
    		Inhibitor
    Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.
    Senexin A hydrochloride
  • HY-130519
    Cdc7-IN-7
    		Inhibitor
    Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
    Cdc7-IN-7
  • HY-B0402B
    Amantadine sulfate
    		Inhibitor
    Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
    Amantadine sulfate
  • HY-153221
    QR-6401
    		Inhibitor
    QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer.
    QR-6401
  • HY-163856
    CDK7-IN-30
    		Inhibitor
    CDK7-IN-30 (Compound 22) is a CDK7 inhibitor (IC50 = 7.21 nM) that effectively inhibits the phosphorylation of RNA Polymerase II and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research.
    CDK7-IN-30
  • HY-172153
    CDK2-IN-41
    		Inhibitor
    CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that exerts anticancer activity by binding to CDK2, thereby inhibiting the cell cycle, inducing cytotoxicity, promoting ROS production, and triggering Apoptosis. CDK2-IN-41 exhibits an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. It holds potential for research in AML-related cancer therapy.
    CDK2-IN-41
  • HY-145394
    CDK7-IN-6
    		Inhibitor
    CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer.
    CDK7-IN-6
  • HY-157297
    CDK-IN-13
    		Inhibitor
    CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines.
    CDK-IN-13
  • HY-159155
    CDK2/4-IN-1
    		Inhibitor
    CDK2/4-IN-1 (compound B-4a) is a CDK2/4 inhibitor and a tubulin polymerization inhibitor. CDK2/4-IN-1 can be used in cancer research.
    CDK2/4-IN-1
  • HY-169994
    BC13
    		Inhibitor
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels.
    BC13
  • HY-147601
    CDK7-IN-16
    		Inhibitor
    CDK7-IN-16 (compound 9) is a potent CDK 7 inhibitor with an IC50 range of 1 ~ 10 nM. CDK7-IN-16 can be used for researching anticancer, especially the cancer with transcriptional dysregulation.
    CDK7-IN-16
  • HY-147716
    CDK8-IN-6
    		Inhibitor
    CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer.
    CDK8-IN-6
  • HY-146587
    Haspin-IN-2
    		Inhibitor
    Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC50 of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 445 nM and 917 nM, respectively.
    Haspin-IN-2
  • HY-112418
    CDK4/6-IN-18
    		Inhibitor
    CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells.
    CDK4/6-IN-18
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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