Cas No.: | 2270879-17-7 |
Chemical Name: | BRM/BRG1 ATP Inhibitor-1 |
Synonyms: | BRM/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 |
SMILES: | S1C(=CC(C(F)F)=N1)NC(NC1C=C(N=CC=1CO)F)=O |
Formula: | C11H9F3N4O2S |
M.Wt: | 318.274970769882 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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]. |
Target: | IC50: ﹤0.005 µM (BRM, BRG1)[1] |
References: | [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 |