>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

Aloxistatin E64d; E64c ethyl ester

Aloxistatin (E64d) 是可渗透细胞,不可逆的广谱半胱氨酸蛋白酶 (cysteine protease) 抑制剂。Aloxistatin (E64d) 可抑制 MERS-CoV。

货号：
TK0536
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	88321-09-9
生物活性	Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
分子式	C17H30N2O5
分子量	342.43
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 250 mg/mL (699.48 mM; Need ultrasonic)，H2O : 12.5 mg/mL (34.97 mM; Need ultrasonic)
体内研究	Oral administration of Aloxistatin (E64d) to guinea pigs results in a dose-dependent reduction in brain, CSF and plasma Aβ(40) and Aβ(42). Aloxistatin also causes a biphasic dose-dependent reduction in brain CTFβ. Aloxistatin causes a dose-dependent increase in brain sAβPPα. The mean sAβPPα levels are significantly higher than the no dose group for Aloxistatin doses of 5 mg/kg/day or greater with the highest Aloxistatin dose resulting in the maximum increase in sAβPPα of about 54% more than the control group. Similar to the Aβ effect, oral Aloxistatin administration produces a biphasic dose-dependent reduction in brain cathepsin B activity. The minimum effective dose is about 1 mg/kg/day with the highest Aloxistatin dose causing the maximum reduction in brain cathepsin B activity of about 91% lower than that of the control group. Thus, Aloxistatin reduces guinea pig brain cathepsin B activity in a manner which is consistent with the compound inhibiting cathepsin B β-secretase activity. Aloxistatin (E64d) inhibits the increases in the expression of AT1AR and ACE genes in rats. Administration of RNH-6270 or Aloxistatin reduces the increase in the superoxide production of the intramyocardial coronary arteries in HF rats.
体外研究	Inhibition of protease-resistant prion protein (PrP-res) accumulation in ScNB cells by cysteine protease inhibitor Aloxistatin (E64d) with IC50 of 0.5±0.11 μM. For the cell surface PrP-sen detection, PrP-sen is immunoprecipitated from media treated with phosphatidylinositol-specific phospholipase C (PIPLC) to release pulse-S-labeled PrP-sen from the cell surface. Aloxistatin is maintained at 15 μM, respectively, in the labeling media of all but the control cells . Aloxistatin (E64d) (which specifically blocks cysteine proteases, but not serine proteases such as granzymes) is able to completely block turnover of the CatL substrate Z-Phe-Arg-aminomethylcoumarin, when pre-incubated with NK-92 or YT 5 cells. Aloxistatin (E64d) is a broad-spectrum cell-permeable inhibitor of cysteine proteases.
文献	•Cancer Cell. 2021 Mar 8;39(3):423-437.e7. •Signal Transduct Target Ther. 2021 Mar 27;6(1):134. •Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121. •Nat Commun. 2021 Sep 17;12(1):5498. •Nat Commun. 2020 Mar 27;11(1):1620. •Cell Discov. 2021 Dec 14;7(1):119. •Elife. 2021 Jan 4;10:e64508. •Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. •Pharmacol Res. 2021 Dec 1;175:105985. •Front Immunol. 2021 Apr 23;12:642855. •Emerg Microbes Infect. 2022 Jan 6;1-29. •PLoS Pathog. 2021 Mar 4;17(3):e1009370. •Chem Biol Interact. 2021 Feb 25;336:109319. •FASEB J. 2022 Jan;36(1):e22121. •J Virol. 2021 Sep 22;JVI0153721. •Vaccines. 2020 Jan 13;8(1):22. •Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. •Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. •PLoS One. 2019 Dec 30;14(12):e0227278. •Biochem Bioph Res Co. 2020 Sep 10;530(1):292-300. •Mol Med Rep. 2019 Jan;19(1):41-50. •Biosaf Health. 3 January 2022. •bioRxiv. 2021 Jan 22. •bioRxiv. 2020 Jun.
纯度及产品资料	98%

推荐产品