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Cathepsin L inhibitor

Names

[ CAS No. ]:
167498-29-5

[ Name ]:
Cathepsin L inhibitor

[Synonym ]:
z-phe-tyr-cho
z-phe-tyr-aldehyde
cathepsin l inhibitor ii

Biological Activity

[Description]:

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease
Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin

[Target]

Cathepsin L (CTSL)[1]


[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[1]. 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[2].

[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[3].

[References]

[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.

[3]. J T Woo, et al. Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo. Eur J Pharmacol. 1996 Apr 4;300(1-2):131-5.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H26N2O5

[ Molecular Weight ]:
446.49500

[ Exact Mass ]:
446.18400

[ PSA ]:
104.73000

[ LogP ]:
3.93790


Related Compounds