Z-Leu-Leu-Nle-aldehyde

Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

Z-LLNle-CHO (0-5 µM or 0-3 µM; 72 h) results in a dose-dependent decrease in cell viability/proliferation in six breast cancer cell lines[1]. Z-LLNle-CHO shows proteasome inhibitory activity, which contributes to cytotoxicity to MCF-7 cells[1]. Z-LLNle-CHO blocks Akt-mediated pro-survival pathways and induces caspase- and ROS-dependent cell apoptosis in Nalm6 and 697 cells[2]. Cell Viability Assay[1] Cell Line: MCF-7, BT474, T47D, MDA-MB-231, SKBR3, and MDA-MB-468 cells Concentration: 0-5 µM (for MCF-7); 0-3 µM Incubation Time: 72 h Result: Inhibited MCF-7, BT474, T47D, MDA-MB-231, SKBR3, and MDA-MB-468 cells with ED50 values of 3.25, 2.5, 2.4, 1.8, 1.6, and 1.4 μM, respectively. Apoptosis Analysis[2] Cell Line: Precursor-B ALL cells Concentration: 0-2.5 µM Incubation Time: 18-24 h Result: Induced cell apoptosis.

Z-LLNle-CHO (5 mg/kg; s.c.; single daily for 12 days) inhibits engraftment of B-lymphoblasts in precursor-B ALL xenograft model[2]. Animal Model: Female SCID/NOD mice (6-8-week-old; precursor-B ALL xenograft model)[2]. Dosage: 5 mg/kg Administration: Subcutaneous injection; single daily for 12 days Result: Delayed or prevented engraftment of B-lymphoblasts in 50% of the animals comprising the experimental group.