OF-1 is a chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1, BRPF2, BRPF3) that assemble histone acetyltransferase (HAT) complexes of the MYST family members MOZ and MORF.
OF-1 is a chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1, BRPF2, BRPF3) that assemble histone acetyltransferase (HAT) complexes of the MYST family members MOZ and MORF. The BRPF1 protein is the scaffold subunit of the MYST acetyltransferase complex, which plays a crucial roles in DNA repair, recombination and replication as well as transcription activation. OF-1 binds to BRPF1B with a Kd of 100 nM , to BRPF2 with a Kd of 500 nM and to BRPF3 with a Kd of 2.4 mM, and shows >100-fold selectivity against most other bromodomains. The closest off-target effects are against BRD4 (39-fold selectivity) and 50% inhibition of TIF1a at 20 μM. For full characterization details, please see OF-1
on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
| 分子量 | 440.31 |
| 分子式 | C17H18BrN3O4S |
| CAS号 | 919973-83-4 |
| 溶解性（25°C） | DMSO: 5 mg/mL (warmed) |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.2711 mL | 11.3556 mL | 22.7113 mL |
| 5 mM | 0.4542 mL | 2.2711 mL | 4.5423 mL |
| 10 mM | 0.2271 mL | 1.1356 mL | 2.2711 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
[1] Won-Gune Jeong, et al. Removal of 1,2-dichloroethane in groundwater using Fenton oxidation
[2] Bas C Stunnenberg, et al. N-of-1 Trials in Neurology: A Systematic Review
[3] Wanying He, et al. Status of N-of-1 Trials in Chronic Pain Management: A Narrative Review
[4] Suzanne McDonald, et al. N-of-1 Trials in Healthcare
[5] E Mordijck, et al. N-of-1 trials in child and adolescent psychiatry: a closer look at stimulants
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