Hexokinase 2 modulator Comp-1

Tuvatexib (Hexokinase 2 modulator Comp-1) is a potent, selective small molecule modulator of Hexokinase 2 (HK2) interaction with the mitochondria, selectively dissociates HK2 from VDAC1 in vitro with IC50 of 92 nM; does not affect the VDAC1/HK1 complex; dose-dependent reduces mitochondrial-bound HK2 levels in human skin SCC A431 cells with IC50 of 0.8 uM, reduces glycolysis and triggers apoptosis in cancer cells, without affecting hexokinase 1-expressing normal cells; demonstrates anti-cancer activity in UVB-damaged skin model in SKH-1 mice.

References 1. Behar V, et al. J Invest Dermatol. 2018 Jun 14. pii: S0022-202X(18)32056-6. 2. Goldin N, et al. Oncogene. 2008 Aug 7;27(34):4636-43. 3. Krasnov GS, et al. Expert Opin Ther Targets. 2013 Oct;17(10):1221-33. 4. PCT Int. Appl. (2018), WO 2018083705 A1 20180511. View Related Products by Target Hexokinase