GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels.

TRPC3 (rat):5 nM (IC50), TRPC6 (rat):4 nM (IC50)

Nuclear factor of activated T cells (NFAT) activation by Ang II ( angiotensin II) is blocked in a dose dependent manner by GSK255B (0.01, 0.1, and 1 μM) in HEK293T cells overexpressing TRPC3. GSK255B blocks NFAT activation by Ang II in HEK293T cells expressing a mutant TRPC6 channel with T70 and S322 mutated to glutamic acid (SETE)[1]. GSK255B (10 μM) blocks calcium entry stimulated by Phenylephrine (20 μM) in rat neonatal cardiac myocytes. GSK255B dose-dependent blockade of cell hypertrophy signaling triggered by angiotensin II or endothelin-1 in HEK293T cells as well as in neonatal and adult cardiac myocytes[1].