RO2959 hydrochloride is a potent and selectiveCRAC channelinhibitor with anIC₅₀of 402 nM. RO2959 hydrochloride is a potent blocker ofstore operated calcium entry (SOCE)mediated byOrai1/Stim1 channelswith anIC₅₀of 25 nM. RO2959 hydrochloride is also a potent inhibitor ofhumanIL-2production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways^[1][2].

RO2959 inhibits Orai1 and Orai3 with IC₅₀values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC₅₀value of 265 nM^[1].
RO2959 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)^[1].

Solid

C₂₁H₁₉F₂N₅OS.xHCl

1219927-22-6

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)