Background:

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