OK2, a specific inhibitor of the CCN2/EGFR interaction, efficiently blocks CCN2/EGFR interaction through binding to the CT domain of CCN2. OK2 can be used for kidney fibrosis and chronic kidney disease research.
OK2 (0-100 μM; 24 hours) inhibits EGFR activation, STAT3 phosphorylation, and ECM protein synthesis in HK-2 cells[1].
OK2 (50 μg/kg, i.p., for 14 days) blocks CCN2-induced EGFR/STAT3 activation and impede kidney fibrosis in the unilateral ureteric obstruction (UUO) mice model[1].
OK2 (1 mg/kg, s.c.) shows a T1/2 of 0.9 h and Cmax of 1057.8 ng/mL in male Sprague Dawley rats[1].
Pharmacokinetic parameters for OK2 in male Sprague Dawley rats [1]
References:
[1]. Dong J, et.al. Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment. J Med Chem. 2023 Jun 22;66(12):8251-8266.