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BRM014

Chemical Structure : BRM014

CAS No.: 2270879-17-7

BRM014 (BRM-014, Dual BRM and BRG1 inhibitor 14)

Catalog No.: PC-35746Not For Human Use, Lab Use Only.

BRM014 (BRM-014) is a potent, orally active inhibitor of Brahma Homolog (BRM)/SMARCA2 and Brahma-related gene 1 (BRG1) with IC50 of <5 nM for both.

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Biological Activity

BRM014 (BRM-014) is a potent, orally active inhibitor of Brahma Homolog (BRM)/SMARCA2 and Brahma-related gene 1 (BRG1) with IC50 of <5 nM for both.
BRM014 modulates SWI/SNF chromatin-remodeling activity via inhibition of the ATPase activity.
BRM014 downregulates BRM-dependent gene expression and shows antiproliferative activity in a BRG1-mutant-lung-tumor xenograft model.

Physicochemical Properties

M.Wt 318.274
Formula C11H9F3N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea

References

1. Papillon JPN, et al. J Med Chem. 2018 Oct 31. doi: 10.1021/acs.jmedchem.8b01318.
2. Rago F, et al. Mol Cancer Res. 2022 Mar 1;20(3):361-372.

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