產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg
CAS	161710-10-7
別名
化學(xué)名	benzyl ((2R,3R)-3-methyl-1-(((R)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)carbamate
分子式	C20H30N2O4
分子量	362.46
溶解度	≥ 10.8mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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

Notch signaling impinges on many cellular processes, including cell proliferation, differentiation, apoptosis, and maintenance of stem cells. It is also involved in many developmental systems, including neurogenesis, angiogenesis, hematopoiesis, and myogenesis. Deregulation of Notch signaling leads to developmental syndromes and cancer [3]. In order to transmit a signal, Notch receptors undergo a series of proteolytic cleavages after binding their cognate ligands of the Delta-like and Jagged family. γ-Secretase is a large protease complex that cleaves the membrane-bound form of Notch and releases the intracellular domain of the Notch receptor. This step in Notch signaling is pivotal in the activation of this signaling cascade [1] [2].

In vitro: 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 [1]. 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 [3].

In vivo: 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[1]. Notch inhibition using GSI XII (intraperitoneal injection, 5 mg/kg) blocked embryonal rhabdomyosarcoma tumorigenesis in mice[2].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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