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-148530
    YX-2-107
    Degrader 99.22%
    YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph+ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).
    YX-2-107
  • HY-107407
    SB-218078
    Inhibitor 98.30%
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
    SB-218078
  • HY-13231
    CDK9-IN-1
    Inhibitor 98.52%
    CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
    CDK9-IN-1
  • HY-117049
    Leucettine L41
    Inhibitor 98.98%
    Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively). Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model.
    Leucettine L41
  • HY-103221
    MeBIO
    Inhibitor ≥98.0%
    MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.
    MeBIO
  • HY-137432
    Avotaciclib
    Inhibitor 99.72%
    Avotaciclib (BEY1107) is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib can be used in the research of cancer such as pancreatic cancer and lung cancer.
    Avotaciclib
  • HY-122586
    BRD6989
    Inhibitor 99.56%
    BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes.
    BRD6989
  • HY-144971
    dCeMM2
    Degrader 99.25%
    dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.
    dCeMM2
  • HY-152219
    CLK1-IN-2
    Inhibitor 98.15%
    CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for the research of tumour, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza.
    CLK1-IN-2
  • HY-117203A
    CDK12-IN-E9
    Inhibitor 99.71%
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
    CDK12-IN-E9
  • HY-16559
    Riviciclib hydrochloride
    99.08%
    Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.
    Riviciclib hydrochloride
  • HY-129180
    XY028-133
    Inhibitor 98.62%
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.
    XY028-133
  • HY-16297AS
    Abemaciclib-d8
    Inhibitor 99.57%
    Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib-d<sub>8</sub>
  • HY-P2559
    CDK7/9 tide
    99.92%
    CDK7/9 tide is peptide substrate for CDK7 or CDK9.
    CDK7/9 tide
  • HY-145121
    DS96432529
    Inhibitor 99.93%
    DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.
    DS96432529
  • HY-103019B
    (-)-Enitociclib
    Inhibitor 99.85%
    (-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.
    (-)-Enitociclib
  • HY-15889
    AMG 925
    Inhibitor 99.02%
    AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
    AMG 925
  • HY-103712B
    Samuraciclib hydrochloride dihydrate
    Inhibitor 99.08%
    Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
    Samuraciclib hydrochloride dihydrate
  • HY-N1431
    Tabersonine
    Inhibitor 98.14%
    Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
    Tabersonine
  • HY-129336
    Abemaciclib metabolite M20
    Inhibitor
    Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.
    Abemaciclib metabolite M20
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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