OF-1

• CAT Number: I005482
• CAS Number: 919973-83-4
• Molecular Formula: C17H18BrN3O4S
• Molecular Weight: 440.31
• Purity: ≥95%
• Synonyms: 4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxobenzimidazol-5-yl)-2-methylbenzenesulfonamide
• InChI: InChI=1S/C17H18BrN3O4S/c1-10-7-11(18)5-6-16(10)26(23,24)19-12-8-13-14(9-15(12)25-4)21(3)17(22)20(13)2/h5-9,19H,1-4H3
• InChIKey: YUNQZQREIHWDQT-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=C1)Br)S(=O)(=O)NC2=CC3=C(C=C2OC)N(C(=O)N3C)C

OF-1 is a potent pan-BRPF bromodomain (BRD) inhibitor, with IC50 values of 270 nM, 1.2 μM for TRIM24 and BRPF1B, respectively[1][2].
OF-1 (1 μM and 2 μM, 0, 1, 2, and 3 days) causes significant reductions in the number of multinucleated tartrate-resistant acid phosphatase (TRAP) positive cells[1].
OF-1 is the only inhibitor to completely suppress the fusion into multinucleated “osteoclast-like” cells[1].

Reference

[1]. Julia C Meier, et al. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630.
 [Content Brief]

[2]. James Bennett, et al. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J Med Chem. 2016 Feb 25;59(4):1642-7.
 [Content Brief]