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

CDK

Cyclin dependent kinase

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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-50767
    Palbociclib
    Inhibitor 99.94%
    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.
    Palbociclib
  • HY-16297A
    Abemaciclib
    Inhibitor 99.96%
    Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib
  • HY-15777
    Ribociclib
    Inhibitor 99.94%
    RRibociclib (LEE011) is an ATP-competitive and orally active 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
  • HY-12529
    Ro-3306
    Inhibitor 98.68%
    Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
    Ro-3306
  • HY-10492
    Dinaciclib
    Inhibitor 99.36%
    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.
    Dinaciclib
  • HY-X0009
    JSH-009
    Inhibitor
    JSH-009 is a novel, highly selective CDK9 inhibitor critical for regulating transcription elongation. JSH-009 demonstrated significant in vitro and in vivo efficacy against acute myeloid leukemia (AML).
    JSH-009
  • HY-142076A
    CDK4/6-IN-15 hydrochloride
    Inhibitor 99.04%
    CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.
    CDK4/6-IN-15 hydrochloride
  • HY-163944
    LL-K12-18
    LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction of the CDK12-DDB1 complex, stabilizing the CDK12-DDB1 complex and promoting the degradation of cyclin K (EC50=0.37 nM). LL-K12-18 exhibits strong gene transcription inhibition and anti-proliferation effects in tumor cells. LL-K12-18 can be used in cancer research.
    LL-K12-18
  • HY-101563
    GSK3326595
    99.97%
    GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
    GSK3326595
  • HY-10005
    Flavopiridol
    Inhibitor 99.73%
    Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
    Flavopiridol
  • HY-50767A
    Palbociclib monohydrochloride
    Inhibitor 99.98%
    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.
    Palbociclib monohydrochloride
  • HY-30237
    (R)-Roscovitine
    Inhibitor 99.84%
    (R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
    (R)-Roscovitine
  • HY-16297
    Abemaciclib methanesulfonate
    Inhibitor 99.95%
    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib methanesulfonate
  • HY-80013
    THZ1
    Inhibitor 99.84%
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
    THZ1
  • HY-112088
    AZD4573
    Inhibitor 99.98%
    AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.
    AZD4573
  • HY-103618
    THZ531
    Inhibitor 99.86%
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
    THZ531
  • HY-A0065
    Palbociclib isethionate
    Inhibitor 99.99%
    Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate 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 isethionate
  • HY-130250
    SR-4835
    Inhibitor 99.73%
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
    SR-4835
  • HY-12302
    Kenpaullone
    Inhibitor 98.20%
    Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
    Kenpaullone
  • HY-138293
    SY-5609
    Inhibitor 99.66%
    SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity.
    SY-5609
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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