RO2959 (hydrochloride)

RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways^[1][2]. IC50 & Target: IC50: 402 nM (CRAC channel); 25 nM (Orai1/Stim1 channels)^[1]
IL-2 production^[1] In Vitro: RO2959 inhibits Orai1 and Orai3 with IC₅₀ values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC₅₀ value 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].