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

CDK

Cyclin dependent kinase

CDK

Related Products

PDF 1.19 MB

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-160213
    JA397
    		Inhibitor
    JA397 is a potent and selective inhibitor for the TAIRE family with cellular activity ranging from IC50 values of 21 nM to 307 nM.
    JA397
  • HY-50767B
    Palbociclib dihydrochloride
    		Inhibitor
    Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
    Palbociclib dihydrochloride
  • HY-50767D
    Palbociclib orotate
    		Inhibitor
    Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
    Palbociclib orotate
  • HY-103712
    Samuraciclib
    		Inhibitor
    Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects.
    Samuraciclib
  • HY-151409
    CDK1-IN-5
    		Inhibitor
    CDK1-IN-5 (10h) is a selective CDK1 inhibitor with IC50s of 42.19, 188.71 and 354.15 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-5 inhibits growth of cancer cells by affecting cell cycle. CDK1-IN-5 can be used for the research of cancer.
    CDK1-IN-5
  • HY-112243
    Cimpuciclib
    		Inhibitor
    Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity.
    Cimpuciclib
  • HY-130516
    Cdc7-IN-4
    		Inhibitor
    Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
    Cdc7-IN-4
  • HY-151407
    CDK1-IN-3
    		Inhibitor
    CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC50s of 36.8, 305.17 and 369.37 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-3 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-3 can be used for the research of cancer.
    CDK1-IN-3
  • HY-19718
    OTS964
    		Inhibitor
    OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
    OTS964
  • HY-151436
    ZLMT-12
    		Inhibitor
    ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
    ZLMT-12
  • HY-15163
    Zotiraciclib
    		Inhibitor 99.88%
    Zotiraciclib (TG02) is an orally active potent inhibitor of CDK2, JAK2 and FLT3 with IC50 values of 13, 73, and 56 nM, respectively. Zotiraciclib can be used for the research of advanced leukemias and multiple myeloma.
    Zotiraciclib
  • HY-136711
    CDK7-IN-2 hydrochloride hydrate
    		Inhibitor
    CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.
    CDK7-IN-2 hydrochloride hydrate
  • HY-110368
    BS-181 dihydrochloride
    		Inhibitor
    BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
    BS-181 dihydrochloride
  • HY-111537
    rel-AZ5576
    		Inhibitor
    rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.
    rel-AZ5576
  • HY-126244
    CDK4/6-IN-3
    		Inhibitor
    CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.
    CDK4/6-IN-3
  • HY-171334A
    P1D-34
    		Inhibitor
    P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).
    P1D-34
  • HY-130981
    FN-1501-propionic acid
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
    FN-1501-propionic acid
  • HY-130001
    CDK9-IN-9
    		Inhibitor
    CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
    CDK9-IN-9
  • HY-145655
    CDK7-IN-11
    		Inhibitor
    CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.
    CDK7-IN-11
  • HY-149641
    CDK9-IN-29
    		Inhibitor
    CDK9-IN-29 (compound Z11) is a potent CDK9 inhibitor (IC50 = 3.20 nM) with good kinase selectivity. CDK9-IN-29 inhibits cell proliferation and induces apoptosis.
    CDK9-IN-29
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.