产品描述: | AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines |
靶点: |
Phospholipase;Phospholipase; SerineProtease |
体外研究: |
AA26-9 is synthesized based on a piperazine scaffold shown previously to inhibit serine hydrolases in the context of p-nitrophenoxy carbamate. AA26-9-inhibited enzymes originated from diverse functional subclasses of serine hydrolases, including lipases/phospholipases (AADACL1, ABHD6, ESD, FAAH, PAFAH2, LYPLA3), peptidases (APEH, PRCP, CTSA), thioesterases (LYPLA1, LYPLA2), and uncharacterized enzymes (ABHD11, ABHD13, BAT5). AA26-9 inhibits one of its enzyme targets LYPLA1 by covalent carbamoylation of the enzyme’s serine nucleophile (S114). AA26-9 inhibits 1/3 of the over 40 serine hydrolase found in T-cells |
参考文献: |
1. Adibekian A, et al. Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors. Nat Chem Biol. 2011 May 15;7(7):469-78. 2. Borne AL, et al. Deciphering T Cell Immunometabolism with Activity-Based Protein Profiling. Curr Top Microbiol Immunol. 2019;420:175-210. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
6.018 ml |
30.088 ml |
60.176 ml |
5 mM |
1.204 ml |
6.018 ml |
12.035 ml |
10 mM |
0.602 ml |
3.009 ml |
6.018 ml |
50 mM |
0.12 ml |
0.602 ml |
1.204 ml |
|
注意: |
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