For research use only. Not for therapeutic Use.
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride 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].
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].
| Catalog Number | I009089 |
| CAS Number | 2309172-44-7 |
| Synonyms | 2,6-difluoro-N-[5-[4-methyl-1-(5-methyl-1,3-thiazol-2-yl)-3,6-dihydro-2H-pyridin-5-yl]pyrazin-2-yl]benzamide;hydrochloride |
| Molecular Formula | C21H20ClF2N5OS |
| Purity | ≥95% |
| InChI | InChI=1S/C21H19F2N5OS.ClH/c1-12-6-7-28(21-26-8-13(2)30-21)11-14(12)17-9-25-18(10-24-17)27-20(29)19-15(22)4-3-5-16(19)23;/h3-5,8-10H,6-7,11H2,1-2H3,(H,25,27,29);1H |
| InChIKey | GMLSDODALBRLPE-UHFFFAOYSA-N |
| SMILES | CC1=C(CN(CC1)C2=NC=C(S2)C)C3=CN=C(C=N3)NC(=O)C4=C(C=CC=C4F)F.Cl |
| Reference | [1]. Gang Chen, et al. Characterization of a Novel CRAC Inhibitor That Potently Blocks Human T Cell Activation and Effector Functions. Mol Immunol. 2013 Jul;54(3-4):355-67. [2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222. |
