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-112468
    PNU112455A hydrochloride
    Inhibitor 99.56%
    PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
    PNU112455A hydrochloride
  • HY-119966
    CCT036477
    Inhibitor 99.42%
    CCT036477 is a Wnt/β-catenin pathway inhibitor. CCT036477 blocks transcription at β-catenin without altering its levels. CCT036477 inhibits proliferation of various cancer cells, development of embryos, and expression of Wnt target genes (PPARδ, Cyclin D1, TCF4, and ID2).
    CCT036477
  • HY-147651
    β-catenin-IN-4
    Inhibitor 99.84%
    β-catenin-IN-4 (Compound 39) is a β-catenin inhibitor with a Ki of 0.64 μM. β-catenin-IN-4 reduces the protein expression levels of cyclin D1 and c-Myc.
    β-catenin-IN-4
  • HY-130850
    CDK9-IN-10
    Inhibitor 98.09%
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
    CDK9-IN-10
  • HY-151069
    TMX-2039
    Inhibitor 99.42%
    TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC50s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs.
    TMX-2039
  • HY-142696A
    CDK6/PIM1-IN-1 hydrochloride
    Inhibitor 99.38%
    CDK6/PIM1-IN-1 (Compound 51) hydrochloride is an orally active and potent dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 hydrochloride inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 hydrochloride significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
    CDK6/PIM1-IN-1 hydrochloride
  • HY-153556
    GW297361
    Inhibitor 98.13%
    GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively.
    GW297361
  • HY-175282
    ASX-173
    ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers.
    ASX-173
  • HY-N2303
    Eriocalyxin B
    Inhibitor 99.93%
    Eriocalyxin B is a diterpenoid compound that can be isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B exhibits multiple activities, such as anti-cancer, anti-inflammatory, and inhibition of adipogenesis. Eriocalyxin B is capable of inducing apoptosis and autophagy in tumor cells. Eriocalyxin B can be used in the research of cancers, autoimmune diseases, and other conditions.
    Eriocalyxin B
  • HY-15777AR
    Ribociclib hydrochloride (Standard)
    Inhibitor
    Ribociclib (Standard) (LEE011(Standard)) hydrochloride is the analytical standard of Ribociclib hydrochloride (HY-15777A). This product is intended for research and analytical applications. Ribociclib hydrochloride (LEE011 hydrochloride) 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.
    Ribociclib hydrochloride (Standard)
  • HY-103383
    (R)-DRF053 dihydrochloride
    Inhibitor 99.30%
    (R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model.
    (R)-DRF053 dihydrochloride
  • HY-122631
    TG693
    Inhibitor 99.95%
    TG693 is an orally active inhibitor of CLK1. TG693 regulates the mutated exon 31 of the dystrophin gene in vivo. TG693 is used in Duchenne muscular dystrophy (DMD) research.
    TG693
  • HY-N12625
    (R)-(+)-O-Demethylbuchenavianine
    Inhibitor 98.67%
    (R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively.
    (R)-(+)-O-Demethylbuchenavianine
  • HY-15777R
    Ribociclib (Standard)
    Inhibitor
    Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. 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.
    Ribociclib (Standard)
  • HY-103492
    CDK8-IN-1
    Inhibitor 99.77%
    CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.
    CDK8-IN-1
  • HY-15777S
    Ribociclib-d6
    99.9%
    Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). Ribociclib 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.
    Ribociclib-d<sub>6</sub>
  • 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-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-12422B
    (2S,3R)-Voruciclib hydrochloride
    Inhibitor 98.0%
    (2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. Voruciclib is an orally active CDK inhibitor.
    (2S,3R)-Voruciclib hydrochloride
  • HY-145599
    Tanuxiciclib
    Inhibitor 98.0%
    Tanuxiciclib is a cyclin dependent kinase (CDK) inhibitor.
    Tanuxiciclib
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