2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. CDK

CDK

Cyclin dependent kinase

CDK

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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).

CDK Isoform Specific Products:

CDK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15777C
    Ribociclib succinate hydrate
    		Inhibitor 99.94%
    Ribociclib succinate hydrate (LEE011 succinate hydrate) 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 succinate hydrate
  • HY-126675
    AS2863619 free base
    		Inhibitor 99.87%
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
    AS2863619 free base
  • HY-162037
    CDDD11-8
    		Inhibitor 99.62%
    CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation.
    CDDD11-8
  • HY-139980
    CDK9-IN-13
    		Inhibitor 99.94%
    CDK9-IN-13 (compound 38) is potent and selective CDK9 inhibitor, with an IC50 of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents.
    CDK9-IN-13
  • HY-112243A
    Cimpuciclib tosylate
    		Inhibitor 99.65%
    Cimpuciclib tosylate is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity.
    Cimpuciclib tosylate
  • HY-111427
    CDK8/19-IN-1
    		Inhibitor 98.03%
    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-19988
    THZ1-R
    		Inhibitor 98.06%
    THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
    THZ1-R
  • HY-103646
    CK7
    		Inhibitor 99.72%
    CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
    CK7
  • HY-112463
    CDK1-IN-2
    		Inhibitor 98.89%
    CDK1-IN-2 is a CDK1 inhibitor (IC50: 5.8 μM).
    CDK1-IN-2
  • HY-117025A
    Manzamine A hydrochloride
    		Inhibitor 99.66%
    Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
    Manzamine A hydrochloride
  • HY-144691
    PP-C8
    		Inhibitor 99.99%
    PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
    PP-C8
  • HY-148365
    NecroIr1
    		Inhibitor 98.02%
    NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK/cdk4.html" class=" link-product" target=" _blank" >CDK4 expression.
    NecroIr1
  • HY-N5072
    Desmethylglycitein
    		Inhibitor 98.98%
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
    Desmethylglycitein
  • 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-153708
    SGC-CLK-1
    		Inhibitor 99.12%
    SGC-CLK-1 is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. SGC-CLK-1 can inhibit the growth of melanoma and glioblastoma cells.
    SGC-CLK-1
  • HY-50767R
    Palbociclib (Standard)
    		Inhibitor
    Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
    Palbociclib (Standard)
  • 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-100429
    CAN508
    		Inhibitor 99.59%
    CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
    CAN508
  • HY-168555
    YJ1206
    		Degrader
    YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker).
    YJ1206
  • HY-102039
    CDK9-IN-8
    		Inhibitor 99.65%
    CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.
    CDK9-IN-8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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