RO2959 Hydrochloride

CAS NO.：1219927-22-6
Empirical Formula: C21H20ClF2N5OS
Molecular Weight: 463.93
Update Date: 2026-07-16 07:06:08

What is RO2959 Hydrochloride?

Biological Activity

RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with IC50 of 402 nM. It is a potent blocker of Orai1/Stim1 channel-mediated calcium storage entry (SOCE) with IC50 of 25 nM. It is also a potent inhibitor of human IL-2 production, effectively blocking T cell receptor-triggered gene expression and T cell functional pathways.

in vitro

RO2959 hydrochloride inhibits Orai1 and Orai3 with IC ₅₀ values of 25 nM and 530 nM, respectively. It blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC < sub> 50 value of 265 nM.
It is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4 ⁺ T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction ).