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

CDK

Cyclin dependent kinase

CDK

Related Products

PDF 1.19 MB

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-162293
    CDK8-IN-14
    		Inhibitor
    CDK8-IN-14 (compound 12) inhibits CDK8 with an IC50 value of 39.2 nM and has anti-AML cell proliferation activity (molm-13 GC50 = 0.02±0.01μM, MV4-11 GC50 = 0.03±0.01μM).
    CDK8-IN-14
  • HY-161708
    PROTAC FLT3/CDKs degrader-1
    		Degrader
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1
  • HY-164399
    SST0116CL1
    		Degrader
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth.
    SST0116CL1
  • HY-157980
    CDK9-IN-32
    		Inhibitor
    CDK9-IN-32 (compound 006-3) is a CDK9 inhibitor.
    CDK9-IN-32
  • HY-143258
    CDK4/6-IN-8
    		Inhibitor
    CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC50 values of 5.01 nM and 3.97 nM, respectively.
    CDK4/6-IN-8
  • HY-156296
    CDK9-Cyclin T1 PPI-IN-1
    		Inhibitor
    CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model.
    CDK9-Cyclin T1 PPI-IN-1
  • HY-171786
    CDK12-IN-8
    		Inhibitor
    CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer.
    CDK12-IN-8
  • HY-111931
    Indirubin-3'-monoxime-5-sulphonic acid
    		Inhibitor
    Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.
    Indirubin-3'-monoxime-5-sulphonic acid
  • HY-123668
    KM05382
    		Inhibitor
    KM05382 serves as an inhibitor of CDK9 and reduces the transcription of GAPDH.
    KM05382
  • HY-150213
    ODN BW001
    		Inhibitor
    ODN BW001 is an oligodeoxynucleotide (ODN). ODN BW001 plays a regulatory role in the proliferation and activation of osteoblast.
    ODN BW001
  • HY-P11013
    p27
    		Inhibitor
    p27, a CDK inhibitor, is a SCFSkp2/Cks1 substrate. p27 can be used for the study of cancer.
    p27
  • HY-156470
    Multi-kinase-IN-6
    		Inhibitor
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
  • HY-161379
    CLZX-205
    		Inhibitor
    CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC50 of 2.9 nM. CLZX-205 plays an important role in cancer research.
    CLZX-205
  • HY-153426
    CDK9-IN-23
    		Inhibitor
    CDK9-IN-23 (Example 4) is a CDK9 inhibitor with an IC50 of <20 nM.
    CDK9-IN-23
  • HY-145867
    EGFR-IN-45
    		Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-150641
    CDK-IN-9
    		Inhibitor
    CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
    CDK-IN-9
  • HY-18969
    LDC3140
    		Inhibitor
    LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment.
    LDC3140
  • HY-112336
    Aloisine RP106
    		Inhibitor
    Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively.
    Aloisine RP106
  • HY-N12218
    Roccellic acid
    Roccellic acid is a methanol extract of Roccella montagnei with cytotoxicity with an IC50 value of 71.26 μg/ml.
    Roccellic acid
  • HY-111932
    Indirubin-5-sulfonate
    		Inhibitor
    Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
    Indirubin-5-sulfonate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.