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

CDK

Cyclin dependent kinase

CDK

Related Products

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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-153278
    CDK7-IN-21
    		Degrader
    CDK7-IN-21 (compound A22) is a potent CDK7 inhibitor.
    CDK7-IN-21
  • HY-162683
    (S)-PHA533533
    		Inhibitor 98.27%
    (S)-PHA533533 is a cyclin-dependent kinase 2 (CDK2) inhibitor. (S)-PHA533533 shows anti-tumor activity and can induce widespread neuronal UBE3A expression in angelman syndrome model mice.
    (S)-PHA533533
  • HY-139329
    CDK12-IN-6
    		Inhibitor 98.09%
    CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
    CDK12-IN-6
  • HY-149964
    PROTAC CDK9 degrader-7
    		Inhibitor 99.62%
    PROTAC CDK9 degrader-7 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-7 mediates CDK9 degradation via the proteasome.
    PROTAC CDK9 degrader-7
  • HY-W478102
    CDK2-IN-13
    		Inhibitor 98.20%
    CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 of 12 µM. CDK2-IN-13 can be used in research of cancer.
    CDK2-IN-13
  • HY-112462
    Cdk1/2 Inhibitor III
    		Inhibitor 99.69%
    Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively.
    Cdk1/2 Inhibitor III
  • HY-N9561
    Vanicoside B
    		Inhibitor 99.82%
    Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis.
    Vanicoside B
  • HY-155218
    TMX-2172
    		Degrader 99.38%
    TMX-2172 is a PROTACs degrader for CDK2 and CDK5, with the IC50s of 6.5 and 6.8 nM, respectively. TMX-2172 plays an important role in cancer research (Blue: E3 ligase ligand (HY-W008352); Pink: target protein ligand (HY-170748); Black: linker (HY-151072)).
    TMX-2172
  • HY-136726
    CGP-82996
    		Inhibitor 98.12%
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.
    CGP-82996
  • HY-101042
    AG-494
    		Inhibitor 99.31%
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
    AG-494
  • HY-111930
    5-Iodo-indirubin-3'-monoxime
    		Inhibitor 99.50%
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
    5-Iodo-indirubin-3'-monoxime
  • HY-112468
    PNU112455A hydrochloride
    		Inhibitor 99.56%
    PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
    PNU112455A hydrochloride
  • HY-163786
    PROTAC CDK4/6 degrader 1
    		Degrader 98.88%
    PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
    PROTAC CDK4/6 degrader 1
  • HY-12828A
    KH-CB20
    		Inhibitor 99.80%
    KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM).
    KH-CB20
  • HY-125290
    MU1210
    		Inhibitor 99.50%
    MU1210 (compound 12f) is an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 (with IC50 values of 8, 20, and 12 nM respectively), with IC50 for HIPK1 and DYRK2 are 187 and 1309 nM. MU1210 also has favorable pharmacokinetic characteristics (in mice, 10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed).
    MU1210
  • HY-128867
    bio-THZ1
    		Inhibitor 98.06%
    bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
    bio-THZ1
  • HY-162706
    BSJ-5-63
    		Degrader 99.97%
    BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)).
    BSJ-5-63
  • HY-46568
    CDK7/12-IN-1
    		Inhibitor 99.52%
    CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.
    CDK7/12-IN-1
  • HY-P10440
    Cdk5i peptide
    		Inhibitor 99.83%
    Cdk5i peptide is a CDK5 inhibitory peptide with high binding affinity for Cdk5/p25 (Kd of 0.17 μM), which can block the interaction between CDK5 and p25 and reduce the kinase activity of CDK5/p25. Cdk5i peptide can be used in the stud y of neurodegenerative diseases.
    Cdk5i peptide
  • HY-130850
    CDK9-IN-10
    		Inhibitor 98.09%
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
    CDK9-IN-10
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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