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-173147
    CDK2-IN-42
    		Inhibitor
    CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer.
    CDK2-IN-42
  • HY-153704
    CDK4/6-IN-17
    		Inhibitor
    CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model.
    CDK4/6-IN-17
  • HY-177780
    Cyclin K degrader 2
    		Degrader
    Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research.
    Cyclin K degrader 2
  • HY-E70650
    CDC7/DBF4 Recombinant Human Active Protein Kinase
    CDC7/DBF4 Recombinant Human Active Protein Kinaseis a protein kinase that is required for the initiation of DNA replication in eukaryotes.
    CDC7/DBF4 Recombinant Human Active Protein Kinase
  • HY-162529
    CDK4/6-IN-19
    		Inhibitor
    CDK4/6-IN-19 (Compound II-7) is a CDK4/CDK6 inhibitor with IC50 values ​​of 0.2, 5.0 nM, respectively. CDK4/6-IN-19 also inhibits cell proliferation and can be used in cancer research.
    CDK4/6-IN-19
  • HY-19471
    (rac)-ZK-304709
    		Inhibitor
    (rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET.
    (rac)-ZK-304709
  • HY-172620
    LIB3S0280
    		99.89%
    LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 exhibits better anticancer effects in pancreatic cancer cell lines with high TBK1 expression. LIB3S0280 inhibits TBK1 downstream signaling pathways, including PI3K/AKT and NF-κB. LIB3S0280 induces G2/M arrest, apoptosis and cellular senescence. LIB3S0280 can be used for pancreatic ductal adenocarcinoma (PDAC) research.
    LIB3S0280
  • HY-180912
    HS-36
    		Inhibitor
    HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC50 values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia.
    HS-36
  • HY-148651
    CDK2-IN-15
    		Inhibitor
    CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research.
    CDK2-IN-15
  • HY-RS02399
    Cdk8 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Cdk8 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk8 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cdk8 Mouse Pre-designed siRNA Set A
  • HY-145402
    CDK7-IN-7
    		Inhibitor
    CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01).
    CDK7-IN-7
  • HY-E70683
    CDK4/CycD3 Recombinant Human Active Protein Kinase
    CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD3 Recombinant Human Active Protein Kinase is an ortholog of CDK4.
    CDK4/CycD3 Recombinant Human Active Protein Kinase
  • HY-149436
    CDK2/Bcl2-IN-1
    		Inhibitor
    CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells.
    CDK2/Bcl2-IN-1
  • HY-179161
    CDK2-IN-49
    		Inhibitor
    CDK2-IN-49 (Compound 5j) is a CDK2 inhibitor with an IC50 of 0.25 μM. CDK2-IN-49 shows potent activity against CDK7 with an IC50 of 0.14 μM. CDK2-IN-49 induces Apoptosis by raising the levels of p53 and Bax protein expression while reducing the amount of Bcl-2. CDK2-IN-49 inhibits cell division. CDK2-IN-49 can be used in the research of cancer.
    CDK2-IN-49
  • HY-162600
    CDK8-IN-15
    		Inhibitor
    CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases.
    CDK8-IN-15
  • HY-173273
    YJZ5118
    		Inhibitor
    YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer.
    YJZ5118
  • HY-171740
    CDK4-IN-4
    		Inhibitor
    CDK4-IN-4 (example 30) is a selective CDK4 inhibitor (IC50＜10 nM) that can be used in cancer research.
    CDK4-IN-4
  • HY-139986
    CDK7-IN-5
    		Inhibitor
    CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104)).
    CDK7-IN-5
  • HY-E70670
    CDK2/CycA2 Recombinant Human Active Protein Kinase
    CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycA2 Recombinant Human Active Protein Kinase is an ortholog of CDK2.
    CDK2/CycA2 Recombinant Human Active Protein Kinase
  • HY-181036
    CDK12/13 ligand 3
    		Ligand
    CDK12/13 ligand 3 is a CDK12/13 PROTAC ligand. CDK12/13 ligand 3 can be conjugated with E3 ligase ligand (HY-W093272) and linker to synthesize CDK12/13 PROTAC degrader DN1679 (HY-181035). CDK12/13 ligand 3 can be used for cancer research.
    CDK12/13 ligand 3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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