BRM/BRG1 ATP Inhibitor-1

• CAT Number: I019041
• CAS Number: 2270879-17-7
• Molecular Formula: C11H9F3N4O2S
• Molecular Weight: 318.27
• Purity: ≥95%
• Synonyms: 1-[3-(difluoromethyl)-1,2-thiazol-5-yl]-3-[2-fluoro-5-(hydroxymethyl)pyridin-4-yl]urea
• InChI: InChI=1S/C11H9F3N4O2S/c12-8-1-6(5(4-19)3-15-8)16-11(20)17-9-2-7(10(13)14)18-21-9/h1-3,10,19H,4H2,(H2,15,16,17,20)
• InChIKey: CKYCAIAVJIFWPE-UHFFFAOYSA-N
• SMILES: C1=C(C(=CN=C1F)CO)NC(=O)NC2=CC(=NS2)C(F)F

BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active 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. BRM/BRG1 ATP Inhibitor-1 has anticancer activity[1].
BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells[1].?
BRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC50 (absolute AC50) value of 0.01 μM and in RERF-LC-AI cells with an AAC50 value of 0.01 μM[1].
BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner[1].

Reference

[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
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