1366233-41-1

1366233-41-1 structure

Name: GSK2332255B
Chemical Name: GSK2332255B
CAS Number: 1366233-41-1
Molecular Formula: C₁₈H₁₉ClFN₃O₃S
Molecular Weight: 411.88
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2021-10-23 21:05:53
Modify Date: 2024-01-04 16:38:45
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels[1].

Name	GSK2332255B

Description	GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Cardiovascular Disease
Target	rTRPC3:5 nM (IC50) rTRPC6:4 nM (IC50)
In Vitro	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].
References	[1]. Kinya Seo, et al. Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc Natl Acad Sci U S A. 2014 Jan 28;111(4):1551-6.

Molecular Formula	C₁₈H₁₉ClFN₃O₃S
Molecular Weight	411.88