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2376255-48-8

中文名稱 AC-FLTD-CMK
英文名稱 INDEX NAME NOT YET ASSIGNED
CAS 2376255-48-8
分子式 C26H37ClN4O8
分子量 569.05
MOL 文件 2376255-48-8.mol
更新日期 2024/04/14 11:58:26
2376255-48-8 結(jié)構(gòu)式 2376255-48-8 結(jié)構(gòu)式

物理化學(xué)性質(zhì)

沸點(diǎn)962.7±65.0 °C(Predicted)
密度1.275±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at -20°C, protect from light, stored under nitrogen
溶解度Soluble to 1 mg/ml in DMSO
酸度系數(shù)(pKa)3.93±0.19(Predicted)
形態(tài)Solid
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
Ac-FLTD-CMK 是胃泌素 D (GSDMD) 衍生的抑制劑,是炎癥性 caspases 的特異性抑制劑。Ac-FLTD-CMK 對(duì) caspases-1 (IC50 為 46.7 nM),caspases-4 (IC50 為 1.49 μM),caspases-5 (IC50 為 329 nM) 和 caspases-11 均有效,但對(duì)凋亡相關(guān)的 caspase-3 無(wú)效。
靶點(diǎn)

Caspase-1

46.7 nM (IC 50 )

Caspase-4

1.49 μM (IC 50 )

Caspase-5

329 nM (IC 50 )

Caspase-11

體外研究

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.

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