Carbamic acid,N-[(1S)-2-[[(1S)-1-formyl-2-(4-hydroxyphenyl)ethyl]amino]-2-oxo-1-(phenylmethyl)ethyl]-,phenylmethyl ester;Carbamic acid,N-[(1S)-2-[[(1S)-1-formyl-2-(4-hydroxyphenyl)ethyl]amino]-2-oxo-1-(phenylmethyl)...;Z-FY-CHO;Z-PHE-TYR-ALDEHYDE;CATHEPSIN L INHIBITOR II;Z-PHE-TYR-CHO;Z-Phe-Tyr-al
Cas No.
167498-29-5
分子式
C26H26N2O5
分子量
446.50
包装储存
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Z-FY-CHO (Z-Phe-Tyr-CHO) 是一种有效且特异性的组织蛋白酶 L (CTSL) 抑制剂。
生物活性
Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.
性状
Solid
IC50 & Target[1][2]
Cathepsin L (CTSL)
体外研究(In Vitro)
Z-FY-CHO (10 μM, for 1 h) pretreatment alleviated cell death induced by 6-OHDA. Z-FY-CHO inhibits the increase in CTSL protein expression in 6-OHDA-treated SH-SY5Y cells. Treatment with Z-FY-CHO caused more LC3-II and less P62 expression in SH-SY5Y cells treated with 6-OHDA, indicating enhancing autophagy activity, and Z-FY-CHO blocks activation of caspase-3 and PARP. Treatment with the specific cathepsin L inhibitor Z-FY-CHO (10 μM) or transfection with cathepsin L shRNA significantly increased the radiosensitivity of U251 cells. Both suppression and knockdown of cathepsin L in U251 cells increased irradiation-induced DNA damage and G2/M phase cell cycle arrest. Both suppression and knockdown of cathepsin L in U251 cells also increased irradiation-induced apoptosis, as shown by the increased levels of Bax and decreased levels of Bcl-2.
体内研究(In Vivo)
Intraperitoneal administration of Z-FY-CHO (2.5-10 mg/kg) for 4 weeks suppresses bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Z-FY-CHO acts as a bone resorption suppressor through the inhibition of collagen degradation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Lingyun Li, et al. Activated cathepsin L is associated with the switch from autophagy to apoptotic death of SH-SY5Y cells exposed to 6-hydroxydopamine. Biochem Biophys Res Commun. 2016 Feb 12;470(3):579-585.[2]. Qing-qing Zhang, et al. Cathepsin L suppression increases the radiosensitivity of human glioma U251 cells via G2/M cell cycle arrest and DNA damage. Acta Pharmacol Sin. 2015 Sep;36(9):1113-25.
溶解度数据
In Vitro: DMSO : 100 mg/mL (223.96 mM; Need ultrasonic)配制储备液