| 产品描述: | NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins |
| 靶点: |
BRPF1:7.9 nM (IC50);BRPF2:48 nM (IC50);BRPF3:260 nM (IC50);BRD9:310 nM (IC50);BRD4 (BD1):4500 nM (IC50);BRPF1:40 nM (Kd);BRPF2:210 nM (Kd);BRPF3:940 nM (Kd);BRD9:1130 nM (Kd);BRD7:82 nM (IC50) |
| 体外研究: |
NI-42 displays IC50s of 82, 310, and 4500 nM for BRD7, BRD9, and BRD4 (BD1), respectively. It has a Kd of 1130 nM for BRD9. |
| 参考文献: |
1. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.83 ml |
14.149 ml |
28.297 ml |
| 5 mM |
0.566 ml |
2.83 ml |
5.659 ml |
| 10 mM |
0.283 ml |
1.415 ml |
2.83 ml |
| 50 mM |
0.057 ml |
0.283 ml |
0.566 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |