1. Membrane Transporter/Ion Channel
    Immunology/Inflammation
  2. CRAC Channel
    Interleukin Related
  3. RO2959 monohydrochloride

RO2959 monohydrochloride 

Cat. No.: HY-113618B
Handling Instructions

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.

For research use only. We do not sell to patients.

RO2959 monohydrochloride Chemical Structure

RO2959 monohydrochloride Chemical Structure

CAS No. : 2309172-44-7

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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].

IC50 & Target[1]

CRAC channel

402 nM (IC50)

Orai1/Stim1 channels

25 nM (IC50)

IL-2

 

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].

Molecular Weight

463.93

Formula

C₂₁H₂₀ClF₂N₅OS

CAS No.

2309172-44-7

SMILES

O=C(NC1=NC=C(C2=C(C)CCN(C3=NC=C(C)S3)C2)N=C1)C4=C(F)C=CC=C4F.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RO2959 monohydrochlorideCRAC ChannelInterleukin RelatedCalcium release-activated channelsCa2+ release-activated Ca2+ channelsILSOCEIP3T-cellanti-proliferationOrai1Stim1heartfailureIL-2Inhibitorinhibitorinhibit

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RO2959 monohydrochloride
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HY-113618B
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