RO2959 Hydrochloride
RO2959 Hydrochloride Basic information
- Product Name:
- RO2959 Hydrochloride
- Synonyms:
-
- RO2959 Hydrochloride
- RO2959 HCl
- IP3,SOCE,Ca2+ release-activated Ca2+ channels,RO2959 Hydrochloride,Interleukin Related,inhibit,IL-2,Stim1,RO-2959 Hydrochloride,CRAC Channel,anti-proliferation,RO 2959,Calcium release-activated channels,T-cell,RO-2959,Orai1,heart,RO2959,Inhibitor,failure
- SYN5226
- CAS:
- 1219927-22-6
- MF:
- C21H20ClF2N5OS
- MW:
- 463.93
- Mol File:
- 1219927-22-6.mol
RO2959 Hydrochloride Chemical Properties
- storage temp.
- Store at -20°C
RO2959 Hydrochloride Usage And Synthesis
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
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