| 产品描述: | Ac-FLTD-CMK 是消皮素 D (GSDMD) 衍生的抑制剂,是炎症性 caspases 的特异性抑制剂。Ac-FLTD-CMK 对 caspases-1 (IC50 为 46.7 nM),caspases-4 (IC50 为 1.49 μM),caspases-5 (IC50 为 329 nM) 和 caspases-11 均有效,但对凋亡相关的 caspase-3 无效。 |
| 靶点: |
Caspase-1:46.7 nM (IC50);Caspase-4:1.49 μM (IC50);Caspase-5:329 nM (IC50) |
| 体外研究: |
Ac-FLTD-CMK, inhibits GSDMD cleavage by caspases-1, -4, -5, and -11 in vitro, suppresses pyroptosis downstream of both canonical and noncanonical inflammasomes, as well as reduces IL-1β release following activation of the NLRP3 inflammasome in macrophages. By contrast, Ac-FLTD-CMK does not target caspase-3 or apoptotic cell death. Crystal structure of caspase-1 in complex with Ac-FLTD-CMK reveals extensive enzyme-inhibitor interactions involving both hydrogen bonds and hydrophobic contacts. |
| 参考文献: |
1. Jie Yang, et al. Mechanism of gasdermin D recognition by inflammatory caspases and their inhibition by a gasdermin D-derived peptide inhibitor. Proc Natl Acad Sci U S A. 2018 Jun 26;115(26):6792-6797. |
| 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 |
1.757 ml |
8.787 ml |
17.573 ml |
| 5 mM |
0.351 ml |
1.757 ml |
3.515 ml |
| 10 mM |
0.176 ml |
0.879 ml |
1.757 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.351 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。 |