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-169910
    CDK2 degrader 4
    Inhibitor 99.71%
    CDK2 degrader 4 (compound 104) is a potent CDK2 degrader. CDK2 degrader 4 has the potential for the research of cancer.
    CDK2 degrader 4
  • 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-162683
    (S)-PHA533533
    Inhibitor 98.27%
    (S)-PHA533533 is a cyclin-dependent kinase 2 (CDK2) inhibitor. (S)-PHA533533 shows anti-tumor activity and can induce widespread neuronal UBE3A expression in angelman syndrome model mice.
    (S)-PHA533533
  • HY-148214
    CDK2/4/6-IN-2
    Inhibitor 98.20%
    CDK2/4/6-IN-2 is a CKD2/4/6 inhibitor, with IC50 values less than 1 μM, 10 nM, 100 nM respectively.
    CDK2/4/6-IN-2
  • HY-112811
    PROTAC CDK9 degrader-2
    Inhibitor 99.22%
    PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC.
    PROTAC CDK9 degrader-2
  • HY-161828
    JWZ-5-13
    Degrader
    JWZ-5-13 is a potent CDK7 PROTAC degrader that significantly degrades CDK7 via the ubiquitin-proteasome system. JWZ-5-13 has antitumor activity. (Pink: Target protein ligand (HY-161830); Black: linker (HY-Y0925); Blue: E3 ligase ligand (HY-112078)).
    JWZ-5-13
  • 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-121035
    7BIO
    Inhibitor 99.20%
    7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].
    7BIO
  • HY-134622
    GSK-3/CDK5/CDK2-IN-1
    Inhibitor 98.10%
    GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases.
    GSK-3/CDK5/CDK2-IN-1
  • HY-131978
    DB18
    Inhibitor 98.27%
    DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC50 values in the range of 10-30 nM for CLK1, CLK2 and CLK4. DB18 has anti-tumor activity.
    DB18
  • HY-136726
    CGP-82996
    Inhibitor 98.12%
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.
    CGP-82996
  • HY-12828A
    KH-CB20
    Inhibitor 99.80%
    KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM).
    KH-CB20
  • HY-149673
    XPW1
    Inhibitor 99.27%
    XPW1 is a potent and selective CDK9 inhibitor with excellent activity against clear cell renal cell carcinoma (ccRCC) and low toxicity.
    XPW1
  • 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-161723
    LH2-051
    Inhibitor 99.85%
    LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (Ki: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC50 of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease.
    LH2-051
  • HY-78428
    CDK-IN-6
    Inhibitor 99.43%
    CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.
    CDK-IN-6
  • HY-114779
    N9-Isopropylolomoucine
    Inhibitor 99.34%
    N9-Isopropylolomoucine is a mitotic cyclin dependent kinase (CDK) inhibitor. N9-Isopropylolomoucine targets CCNB 1/CDK1 and can be used for cancer research.
    N9-Isopropylolomoucine
  • HY-41076
    Ca2+ channel agonist 1
    Inhibitor 99.71%
    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-111207
    CA224
    Inhibitor 99.94%
    CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.
    CA224
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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