BRM/BRG1 ATP Inhibitor-1 chemical structure
Chemical structureResearch use only
CAT. NO. DC46193Featured

BRM/BRG1 ATP Inhibitor-1

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Product overview

Description & Application

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM[1].

ParameterValue
Chemical NameBRM/BRG1 ATP Inhibitor-1
CAS No.2270879-17-7
SynonymsBRM/BRG1 ATP Inhibitor-1;1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea;TQR0285;Dual BRM and BRG1 inhibitor 14;BDBM50469330
FormulaC11H9F3N4O2S
M.Wt318.274970769882
SMILESS1C(=CC(C(F)F)=N1)NC(NC1C=C(N=CC=1CO)F)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM[1].

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

Target

IC50: ﹤0.005 µM (BRM, BRG1)[1]

References & source

[1]. Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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