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CVT-313 (CAS 199986-75-9)

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Alternate Names:
CVT-313 is also known as Cdk2 Inhibitor III.
Application:
CVT-313 is a cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2.
CAS Number:
199986-75-9
Purity:
≥98%
Molecular Weight:
400.5
Molecular Formula:
C20H28N6O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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CVT-313 is a cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 µM for Cdk2/A and Cdk2/E 4.2 µM for Cdk1/B 215 µM for Cdk4/D1). CVT-313 inhibits other kinases only at much higher concentrations (IC50 > 1.25 mM for MAPK, PKA, and PKC). Additionally, CVT-313 is shown to induce tumor cells growth arrest (IC50 ~1.25-20 µM) in vitro. By halting the cell cycle, CVT-313 suppresses the growth of cancer cells. Furthermore, studies using CVT-313 have explored the interplay between CDK2 and other cellular pathways, including DNA repair mechanisms and apoptosis (programmed cell death).


CVT-313 (CAS 199986-75-9) References

  1. ATP-site directed inhibitors of cyclin-dependent kinases.  |  Gray, N., et al. 1999. Curr Med Chem. 6: 859-75. PMID: 10495356
  2. Histone H1 phosphorylation by Cdk2 selectively modulates mouse mammary tumor virus transcription through chromatin remodeling.  |  Bhattacharjee, RN., et al. 2001. Mol Cell Biol. 21: 5417-25. PMID: 11463824
  3. Inhibition of cyclin-dependent kinase-2 induces apoptosis in human diffuse large B-cell lymphomas.  |  Faber, AC. and Chiles, TC. 2007. Cell Cycle. 6: 2982-9. PMID: 18156799
  4. Global changes in and characterization of specific sites of phosphorylation in mouse and human histone H1 Isoforms upon CDK inhibitor treatment using mass spectrometry.  |  Deterding, LJ., et al. 2008. J Proteome Res. 7: 2368-79. PMID: 18416567
  5. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing.  |  Gräub, R., et al. 2008. Cell Cycle. 7: 1795-803. PMID: 18583928
  6. CDK2 differentially controls normal cell senescence and cancer cell proliferation upon exposure to reactive oxygen species.  |  Hwang, CY., et al. 2012. Biochem Biophys Res Commun. 425: 94-9. PMID: 22819841
  7. Critical reanalysis of the methods that discriminate the activity of CDK2 from CDK1.  |  Sakurikar, N. and Eastman, A. 2016. Cell Cycle. 15: 1184-8. PMID: 26986210
  8. A novel and effective inhibitor combination involving bortezomib and OTSSP167 for breast cancer cells in light of label-free proteomic analysis.  |  Okur, E. and Yerlikaya, A. 2019. Cell Biol Toxicol. 35: 33-47. PMID: 29948483
  9. Differential Sensitivity to CDK2 Inhibition Discriminates the Molecular Mechanisms of CHK1 Inhibitors as Monotherapy or in Combination with the Topoisomerase I Inhibitor SN38.  |  Warren, NJH., et al. 2019. ACS Pharmacol Transl Sci. 2: 168-182. PMID: 32259055
  10. Structure of cyclin-dependent kinase 2 (CDK2) in complex with the specific and potent inhibitor CVT-313.  |  Talapati, SR., et al. 2020. Acta Crystallogr F Struct Biol Commun. 76: 350-356. PMID: 32744246
  11. Identification of selective cyclin-dependent kinase 2 inhibitor from the library of pyrrolone-fused benzosuberene compounds: an in silico exploration.  |  Singh, R., et al. 2022. J Biomol Struct Dyn. 40: 7693-7701. PMID: 33749525
  12. A network pharmacology approach to investigate the anticancer mechanism of cinobufagin against hepatocellular carcinoma via downregulation of EGFR-CDK2 signaling.  |  Yang, AL., et al. 2021. Toxicol Appl Pharmacol. 431: 115739. PMID: 34619160
  13. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation.  |  Brooks, EE., et al. 1997. J Biol Chem. 272: 29207-11. PMID: 9360999

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CVT-313, 1 mg

sc-221445
1 mg
$104.00

CVT-313, 5 mg

sc-221445A
5 mg
$416.00

CVT-313, 50 mg

sc-221445B
50 mg
$2601.00