1. Cell Cycle/DNA Damage
  2. CDK

CDK

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 Related Products (448):

Cat. No. Product Name Effect Purity
  • HY-16297A
    Abemaciclib Inhibitor 99.83%
    Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-15777
    Ribociclib Inhibitor 99.98%
    Ribociclib (LEE01) 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[1].
  • HY-50767
    Palbociclib Inhibitor
    Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib 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[1][3][4].
  • HY-50767A
    Palbociclib monohydrochloride Inhibitor
    Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride 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[1][3][4].
  • HY-10492
    Dinaciclib Inhibitor 99.44%
    Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively[1].
  • HY-149819
    CDK/HDAC-IN-3 Inhibitor
    CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) [1].
  • HY-149974
    CDK8-IN-13 Inhibitor
    CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity[1].
  • HY-153443
    CDK4-IN-2 Inhibitor
    CDK4-IN-2 (A17) is a CDK4 inhibitor, with Ki and IC50 values of <10 nM. Used in cancer research[1].
  • HY-103019
    Enitociclib Inhibitor
    Enitociclib ((+)-Enitociclib) is an enanthiomer of BAY-1251152 with rotation (+). Enitociclib is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. Enitociclib has anti-tumour activity[1][2].
  • HY-101257B
    YKL-5-124 TFA Inhibitor 99.44%
    YKL-5-124 TFA 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 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1].
  • 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[1].
  • HY-12445
    Asnuciclib Inhibitor 99.76%
    Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4].
  • HY-50943
    AT7519 Hydrochloride Inhibitor 99.42%
    AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
  • 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[1][2].
  • HY-101467
    Trilaciclib Inhibitor
    Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
  • HY-137346
    DD-03-156 98.52%
    DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17[1].
  • 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[1].
  • HY-143587
    CDK7-IN-2 Inhibitor
    CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1)[1].
  • 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[1].
  • 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[1].