| 产品描述： | MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice |
| 靶点： |
BRD4-BD1:77 nM (Ki);BRD2-BD1:83 nM (Ki);BRD3-BD1:110 nM (Ki);BRD3-BD2:200 nM (Ki);BRD2-BD2:240 nM (Ki);BRD4-BD2:718 nM (Ki) |
| 体内研究： |
Reconstitution with naïve CD4+CD45RBhi cells isolated from spleen and lymph nodes of C57BL/6 mice, Rag1-/- mice begin losing weight after 4 week. MS402 (10 mg/kg; intraperitoneally twice a week for 3 weeks) shows much less weight loss. Animal Model: C57BL/6 mice, Rag1-/- mice with T-cell transfer-induced colitis model Dosage: 10 mg/kg Administration: Intraperitoneally twice a week for 3 weeks Result: Showed much less weight loss. |
| 参考文献： |
1. Cheung K, et al. BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957. |
| 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 |
2.697 ml |
13.483 ml |
26.966 ml |
| 5 mM |
0.539 ml |
2.697 ml |
5.393 ml |
| 10 mM |
0.27 ml |
1.348 ml |
2.697 ml |
| 50 mM |
0.054 ml |
0.27 ml |
0.539 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
