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-147054
    WEE1-IN-5
    Inhibitor 99.46%
    WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. WEE1-IN-5 can be used for researching anticancer.
    WEE1-IN-5
  • HY-12871B
    Atuveciclib
    Inhibitor 99.75%
    Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9/CycT1 with an IC50 of 13 nM.
    Atuveciclib
  • HY-13914
    Roniciclib
    Inhibitor 98.09%
    Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.
    Roniciclib
  • HY-128669
    Abemaciclib metabolite M2
    Inhibitor 99.75%
    Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s of 1.2 and 1.3 nM, respectively. Anti-cancer activity.
    Abemaciclib metabolite M2
  • HY-15275
    BMS-265246
    Inhibitor 99.59%
    BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.
    BMS-265246
  • HY-B0766
    Bicyclol
    99.91%
    Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.
    Bicyclol
  • HY-N6742
    Borrelidin
    Inhibitor 99.80%
    Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells. Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively.
    Borrelidin
  • HY-18629
    SU9516
    Inhibitor 99.85%
    SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
    SU9516
  • HY-12280
    THZ2
    Inhibitor 99.03%
    THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.
    THZ2
  • 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.
    Asnuciclib
  • HY-117535
    CDK2-IN-4
    Inhibitor 99.85%
    CDK2-IN-4 (compound 73) is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).
    CDK2-IN-4
  • HY-13266A
    BS-181 hydrochloride
    Inhibitor 99.93%
    BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
    BS-181 hydrochloride
  • HY-141687
    NSC 107512
    Inhibitor 99.97%
    NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors.
    NSC 107512
  • HY-12624
    Narazaciclib
    Inhibitor 98.66%
    Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM.
    Narazaciclib
  • HY-10424
    Milciclib
    Inhibitor 99.90%
    Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
    Milciclib
  • HY-N0404
    Sinigrin
    Inhibitor 99.97%
    Sinigrin (Allyl-glucosinolate) is an orally active glucosinolate found in cruciferous plants. Sinigrin possesses multiple activities such as anti-cancer, antibacterial, antifungal, anti-inflammatory, antioxidant, and inhibition of fat synthesis. Sinigrin can be used in the research of tumors, inflammatory, and metabolic diseases.
    Sinigrin
  • HY-18340A
    (R)-CR8 trihydrochloride
    Inhibitor 98.95%
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
    (R)-CR8 trihydrochloride
  • HY-103082
    CLK1-IN-1
    Inhibitor 98.55%
    CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.
    CLK1-IN-1
  • HY-15504
    RGB-286638
    Inhibitor 99.70%
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638
  • HY-129478
    TC11
    Activator 99.55%
    TC11 is a MCL1 degrader and Caspase-9 and CDK1 activator. TC11 functions as a phenylacetylamide derivative and is structurally related to immunomodulatory active molecules. TC11 induces degradation of MCL1 leading to apoptotic death during prolonged mitotic arrest.
    TC11
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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