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OF-1
- Soluble in DMSO
- MF: C17H18BrN3O4S
- MW: 440.31
Description
OF-1 is a bromodomain inhibitor selective for BRPF family proteins, with strongest activity at BRPF1 and BRPF2. It blocks acetyl-lysine reader function in chromatin-associated regulatory complexes.
BRPF bromodomains participate in histone acetylation reader complexes that influence transcription, lineage programs and epigenetic regulation. OF-1 is useful for studying BRPF1/2 biology and comparing BRPF-selective inhibition with broader BET bromodomain pharmacology.
Key Features
- BRPF bromodomain inhibitor
- Reported Kd values: 100 nM for BRPF1B, 500 nM for BRPF2 and 2.4 µM for BRPF3
- High selectivity over many non-BRPF bromodomains
- Targets chromatin reader function rather than catalytic enzymes
Applications
- Bromodomain pharmacology
- Epigenetic reader-domain research
- BRPF1/BRPF2 selectivity studies
- Chromatin and transcriptional regulation assays
More Information
| Parent CAS No. | 919973-83-4 |
|---|---|
| Chemical Name | 4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methylbenzenesulfonamide |
| SMILES | C1(S(NC2=C(OC)C=C3N(C)C(=O)N(C)C3=C2)(=O)=O)=CC=C(Br)C=C1C |
| MFCD | N.A. |
| 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 |
| CID | 35397514 |
| Short Description | BRPF inhibitor |
References
- J 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.
- AH Miah et al. Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists. Bioorg Med Chem. 2014 Aug 1;22(15):4298-311.
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