Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) 是一种γ-Secretase抑制剂 I。Z-LLNle-CHO 通过阻断Akt介导的促生存途径并诱导caspase和 ROS 依赖性细胞凋亡。Z-LLNle-CHO 可用于癌症的研究,如乳腺癌和白血病。
生物活性 | Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is aγ-secretaseinhibitor I. Z-LLNle-CHO inducescaspaseand ROS-dependentapoptosisby blocking theAkt-mediated pro-survival pathway. Z-LLNle-CHO can be used incancerresearch, such as breastcancerand leukaemia[1][2]. |
体外研究 (In Vitro) | 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 ED50values 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. |
|
体内研究 (In Vivo) | 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. |
|
分子量 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |