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-12422A
    Voruciclib hydrochloride
    Inhibitor 99.26%
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
    Voruciclib hydrochloride
  • HY-137432A
    Avotaciclib trihydrochloride
    Inhibitor 99.60%
    Avotaciclib (BEY1107) trihydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib trihydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib trihydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer.
    Avotaciclib trihydrochloride
  • HY-168518
    PROTAC CDK9 degrader-9
    Degrader 99.25%
    PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research.
    PROTAC CDK9 degrader-9
  • HY-143587
    CDK7-IN-2
    Inhibitor 98.93%
    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).
    CDK7-IN-2
  • HY-112280
    Crozbaciclib
    Inhibitor 99.94%
    Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
    Crozbaciclib
  • HY-122665
    HTH-01-091
    Inhibitor 99.81%
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.
    HTH-01-091
  • HY-111427
    CDK8/19-IN-1
    Inhibitor 98.08%
    CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
    CDK8/19-IN-1
  • HY-130852
    CDK9-IN-11
    Inhibitor
    CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628).
    CDK9-IN-11
  • HY-178861
    dCDK9-202
    Degrader 99.25%
    dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).
    dCDK9-202
  • HY-P2480
    Histone H1-derived Peptide
    99.92%
    Histone H1-derived Peptide is a phosphopeptide and the peptide substrates containes a sequence in accordance with the optimal recognition motif for CDK, can be used to detecting CDK1-cyclinB1 enzyme activity.
    Histone H1-derived Peptide
  • HY-116871
    YKL-1-116
    Inhibitor 98.67%
    YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7WT and Cdk7as, although Cdk7as is relatively resistant to this compound as well.
    YKL-1-116
  • HY-112462
    Cdk1/2 Inhibitor III
    Inhibitor 99.69%
    Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively.
    Cdk1/2 Inhibitor III
  • HY-100600
    BGG463
    Inhibitor 98.0%
    BGG463 (K03859) is an orally active type II CDK2 inhibitor.
    BGG463
  • HY-111930
    5-Iodo-indirubin-3'-monoxime
    Inhibitor 98.12%
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
    5-Iodo-indirubin-3'-monoxime
  • HY-100950
    ABC1183
    Inhibitor 99.62%
    ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.
    ABC1183
  • HY-115714
    CDK9-IN-12
    Inhibitor 99.65%
    CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
    CDK9-IN-12
  • HY-13661
    7-Hydroxystaurosporine
    Activator
    7-Hydroxystaurosporine (UCN-01), a derivative of Staurosporine (HY-15141), is a selective protein kinase C (PKC) inhibitor with antitumor activity. 7-hydroxystaurosporine induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, suppresses invasion and migration in glioblastoma cells. 7-Hydroxystaurosporine exhibits efficacy in breast cancer xenograft mouse models. 7-Hydroxystaurosporine can be used for colon carcinoma, breast cancer, glioblastoma and leukemia research.
    7-Hydroxystaurosporine
  • HY-41076
    Ca2+ channel agonist 1
    Inhibitor 98.87%
    Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
    Ca2+ channel agonist 1
  • HY-123045
    PNU-292137
    Inhibitor 99.95%
    PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model.
    PNU-292137
  • HY-162683
    (S)-PHA533533
    Inhibitor 98.27%
    (S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC50 values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome.
    (S)-PHA533533
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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