OF-1 是一种有效的泛 BRPF 溴结构域 (BRD) 抑制剂，对 TRIM24 和 BRPF1B 的 IC50 值分别为 270 nM 和 1.2 μM。
| Cas No. | 919973-83-4 |
| 化学名 | 4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methylbenzenesulfonamide |
| Canonical SMILES | CN1C2=C(C=C(OC)C(NS(=O)(C3=C(C)C=C(Br)C=C3)=O)=C2)N(C)C1=O |
| 分子式 | C17H18BrN3O4S |
| 分子量 | 440.31 |
| 溶解度 | ≥ 14.55mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor (Kd value = 100nM and 500 nM, respectively; >100-fold selectivity over majority of other bromodomains).
BRPF (BRomodomain and PHD Finger containing) protein family are scaffolding proteins that assembles MYST histone acetyltransferase complexes. MYST complexes play important role in DNA repair, recombination, replication and transcription activation.
In cellular thermal shift assay (CETSA) of full length BRPF1B, OF-1 enhanced thermal stability at 1 µM. In BRPF2 FRAP assay, OF-1 showed accelerated FRAP recovery at 5µM. OF-1 exhibited modest general cytotoxicity.
References:
[1]. OF-1 - A chemical probe for BRPF bromodomains. (2010, October 13). SGC. Retrieved from http://www.thesgc.org/chemical-probes/OF-1 |
