Ac-FLTD-CMK
作者：齊岳
發(fā)布時(shí)間：2023-08-28
09:04:45
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Ac-FLTD-CMK
產(chǎn)品描述：
| 產(chǎn)品描述 | Ac-FLTD-CMK is an inhibitor derived from abscisicin D (GSDMDD) with specific inhibitory effects on inflammatory caspases. ac-FLTD-CMK showed inhibitory effects on caspases-1, caspases-4 and caspases-11 with IC50s of 46.7 nM, 1.49 μM and 329 nM, respectively. Ac-FLTD-CMK showed potency against caspases-1, caspases-4 and caspases-11, but not against apoptosis-associated caspase-3. |
| 靶點(diǎn)活性 | Caspase-1:46.7 nM (IC50), Caspase-5:329 nM (IC50), Caspase-4:1.49μM (IC50) |
| 體外活性 | 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.[1] |
| 分子量 | 569.05 |
| 分子式 | C26H37ClN4O8 |
| CAS No. | 2376255-48-8 |
存儲(chǔ)
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 90.0 mg/mL (158.2 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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