Z-Ile-Leu-aldehyde,161710-10-7

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YZ剂描述：

产品名称：Z-Ile-Leu-aldehyde

产品别名：Z-IL-CHO；GSI-XII；γ-Secretase inhibitor XII

英文别名：Z-IL-CHO;GSI-XII;γ-Secretase inhibitor XII

靶点：Secretase

CAS：161710-10-7

纯度：98%

外观：solid

保存方法：Store at -20°C

描述：

Z-Ile-Leu-aldehyde (gamma-Secretase inhibitor XII /GSI XII, Z-IL-CHO) is a potent gamma-Secretase inhibitor and Notch signaling inhibitor.

溶解性：DMSO : ≥ 41 mg/mL (113.12 mM)

体外研究：

GSI XII (10~15 µM) blocked the Notch signaling, reduced cell viability and induced apoptosis in MOPC315.BM murine multiple myeloma cells in vitro. GSI XII (10 µM) impaired murine osteoclast differentiation of receptor activator of NF-κB ligand (RANKL)-stimulated RAW264.7 murine monocyte/macrophage cell line. GSI XII (8 μM ~ 15 μM) potently triggered an apoptotic response through inhibition of Notch activity in the breast cancer cells. GSI XII also targets mammary cancer stem-like cells because it dramatically prevented in vitro mammosphere formation.

体内研究：Notch inhibition through GSI XII (intraperitoneal injection, 10 mg/kg) reduced myeloma-specific paraprotein levels, bone loss and diminished osteolytic lesions in the MOPC315.BM mice model. Notch inhibition using GSI XII (intraperitoneal injection, 5 mg/kg) blocked embryonal rhabdomyosarcoma tumorigenesis in mice.

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