2309172-44-7

2309172-44-7 structure
2309172-44-7 structure
  • Name: RO2959 monohydrochloride
  • Chemical Name: RO2959 monohydrochloride
  • CAS Number: 2309172-44-7
  • Molecular Formula: C21H20ClF2N5OS
  • Molecular Weight: 463.93
  • Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
  • Create Date: 2020-10-26 11:20:24
  • Modify Date: 2025-08-26 11:36:40
  • 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].

Name RO2959 monohydrochloride
Description 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].
Related Catalog
Target

IL-2

CRAC channel:402 nM (IC50)

Orai1/Stim1 channels:25 nM (IC50)

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].
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.

[2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222.

Molecular Formula C21H20ClF2N5OS
Molecular Weight 463.93
Hazard Codes Xi
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