2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-157297
    CDK-IN-13
    		Inhibitor
    CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines.
    CDK-IN-13
  • HY-159155
    CDK2/4-IN-1
    		Inhibitor
    CDK2/4-IN-1 (compound B-4a) is a CDK2/4 inhibitor and a tubulin polymerization inhibitor. CDK2/4-IN-1 can be used in cancer research.
    CDK2/4-IN-1
  • HY-W1047040
    CDK2/4 ligand 1
    		Inhibitor
    CDK2/4 ligand 1 is a ligand for target protein for PROTACs, which targets CDK2/4. CDK2/4 ligand 1 can be used for synthesis of PROTAC CDK2/4 Degrader-1 (HY-179688).
    CDK2/4 ligand 1
  • HY-114248
    AGM-130
    		Inhibitor
    AGM-130 is a cyclin-dependent kinase (CDK) inhibitor. AGM-130 exhibits antitumor activity.
    AGM-130
  • HY-169994
    BC13
    		Inhibitor
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels.
    BC13
  • HY-147601
    CDK7-IN-16
    		Inhibitor
    CDK7-IN-16 (compound 9) is a potent CDK 7 inhibitor with an IC50 range of 1 ~ 10 nM. CDK7-IN-16 can be used for researching anticancer, especially the cancer with transcriptional dysregulation.
    CDK7-IN-16
  • HY-147716
    CDK8-IN-6
    		Inhibitor
    CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer.
    CDK8-IN-6
  • HY-181906
    ZnPc-PEG2-VH032
    		Inhibitor
    ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC).
    ZnPc-PEG2-VH032
  • HY-146587
    Haspin-IN-2
    		Inhibitor
    Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC50 of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 445 nM and 917 nM, respectively.
    Haspin-IN-2
  • HY-E70678
    CDK3/CycE1 Recombinant Human Active Protein Kinase
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycE1 Recombinant Human Active Protein Kinase is an ortholog of CDK3.
    CDK3/CycE1 Recombinant Human Active Protein Kinase
  • HY-170815
    CDK4/9-IN-1
    		Inhibitor
    CDK4/9-IN-1 (Compound 29) is a selective dual CDK4/9 inhibitor with IC50 values of 23 nM and 12 nM, respectively. CDK4/9-IN-1 is promising for research of cancers.
    CDK4/9-IN-1
  • HY-143430
    (S)-LY3177833
    		Inhibitor
    (S)-LY3177833 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. (S)-LY3177833 shows broad in vitro anticancer activity.
    (S)-LY3177833
  • HY-168444
    CDK4/6-IN-23
    		Inhibitor
    CDK4/6-IN-23 (Compound 42) is a potent and selective CDK4/6 inhibitor, with an IC50 of 11 nM for CDK6. CDK4/6-IN-23 can significantly activate immune cells and promote the production of IL-3. CDK4/6-IN-23 has dual myeloprotective and immunomodulatory effects in 5-FU (HY-90006) chemotherapy mice.
    CDK4/6-IN-23
  • HY-E70690
    CDK8/CycC Recombinant Human Active Protein Kinase
    CDK8 modulates the transcriptional output from distinct transcription factors involved in oncogenic control, including the Wnt/β-catenin pathway, Notch, p53, and transforming growth factor β. Abnormal activity ofCDK8 along with its partner protein cyclin C (CycC) is a common feature of many diseases including colorectal cancer. CDK8/CycC Recombinant Human Active Protein Kinase can be used to study the function of CDK8/CycC.
    CDK8/CycC Recombinant Human Active Protein Kinase
  • HY-147387
    DSS30
    		Inhibitor
    DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursor protein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    DSS30
  • HY-183771
    CDK4/6-IN-28
    		Inhibitor
    CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC50 values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer.
    CDK4/6-IN-28
  • HY-RS02380
    CDK3 Human Pre-designed siRNA Set A
    		Inhibitor

    CDK3 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CDK3 Human Pre-designed siRNA Set A
  • HY-185164
    Anticancer agent 302
    		Degrader
    Anticancer agent 302 (Example 1) is an anticancer agent. Anticancer agent 302 has a DC50 value of 199 nM for Cyclin E1 and an IC50 value of 133 nM for pRB. Anticancer agent 302 can be used for tumor research.
    Anticancer agent 302
  • HY-156115
    EGFR/CDK2-IN-3
    		Inhibitor
    EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM.
    EGFR/CDK2-IN-3
  • HY-169633
    CDK8-IN-17
    		Inhibitor
    CDK8-IN-17 (Compound WS-2) is a CDK8 inhibitor with an IC50 value of 9 nM, which can be used in cancer research.
    CDK8-IN-17
Art. -Nr. Produktname / Synonyms Species Source
Art. -Nr. Produktname / Synonyms Application Reactivity
CDK Isoform Comparison

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