RO2959 hydrochloride 是选择性CRAC通道抑制剂,IC50为 402 nM。它是人IL-2产生的有效抑制剂,有效阻断 T 细胞受体触发的基因表达和 T 细胞功能途径。它是由Orai1/Stim1通道介导的钙存储进入的有效阻滞剂,IC50为 25 nM。
产品描述
RO2959 hydrochloride is a potent and selective inhibitor of CRAC channel(IC50: 402 nM). It is also a potent inhibitor of human IL-2.
体外活性
RO2959 is a potent SOCE inhibitor that blocked 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 TCR stimulation or thapsigargin treatment. RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction).
Cas No.
1219927-22-6
分子式
C21H20ClF2N5OS
分子量
463.93
别名
RO2959 HCl
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years