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OF-1
Axon 2442
CAS:
919973-83-4
Purity:
99%
- Soluble in DMSO
- MF: C17H18BrN3O4S
- MW: 440.31
Description
Potent Bromodomain inhibitor with selectivity for BRPF1 and BRPF2 (Kd values 100 nM, 500 nM, and 2.4 μM for BRPF1B, BRPF2, and BRPF3, respectively). Selectivity against other bromodomains is very good, in general >100-fold. The closest off-target effects are against BRD4 (39-fold selectivity) and TIF1a (50% inhibition at 20 µM. OF-1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay.
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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