OF-1 is a chemical probe for BRPF bromodomains. OF-1 has been shown to bind to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 uM (ITC). 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 in the alphascreen). 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. It shows modest general cytotoxicity. (http://www.thesgc.org/chemical-probes/OF-1).
MedKoo Cat#: 407282
Name: OF-1
CAS#: 19973-83-4
Chemical Formula: C17H18BrN3O4S
Exact Mass: 439.0201
Molecular Weight: 440.31
Elemental Analysis: C, 46.37; H, 4.12; Br, 18.15; N, 9.54; O, 14.53; S, 7.28
The following data is based on the product molecular weight 440.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
