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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]. | [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 ). | [target]
| CRAC channel 402 nM (IC 50 ) | Orai1/Stim1 channels 25 nM (IC 50 ) | IL-2 | | [IC 50]
CRAC channel: 402 nM (IC50); Orai1/Stim1 channels: 25 nM (IC50); IL-2 | [storage]
Store at -20°C | [References]
[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. DOI:10.1016/j.molimm.2012.12.011
[2] Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222. DOI:10.3389/fphar.2017.00222 |
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Novachemistry
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https://www.novachemistry.com/ |
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