ChemicalBook--->CAS DataBase List--->1219927-22-6

1219927-22-6

1219927-22-6 Structure

1219927-22-6 Structure
IdentificationBack Directory
[Name]

RO2959 Hydrochloride
[CAS]

1219927-22-6
[Synonyms]

RO2959 HCl
RO2959 Hydrochloride
[Molecular Formula]

C21H20ClF2N5OS
[MOL File]

1219927-22-6.mol
[Molecular Weight]

463.931
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
Hazard InformationBack Directory
[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

[storage]

Store at -20°C
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