| Bioactivity | 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 [1][2]. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| Name | AA26-9 | ||||||||||||
| CAS | 1312782-34-5 | ||||||||||||
| Formula | C7H10N4O | ||||||||||||
| Molar Mass | 166.18 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |