2891574-93-7

EF-4-177 is an orally active and allosteric CDK2 inhibitor with the IC50 of 87 nM. EF-4-177 can disrupt spermatogenesis[1][2].

CDK2/cyclinE: 87 nM (IC₅₀)

[1] Faber EB, et al. Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice. J Med Chem. 2023;66(3):1928-1940. DOI:10.1021/acs.jmedchem.2c01731
[2] Huang Y, et al. Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity. Eur J Med Chem. Published online May 29, 2024. DOI:10.1016/j.ejmech.2024.116547