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GSI-XII

Development stage: Unknown
Lead developer: Merck KGaA
Modality: Small Molecules
Administration: Parenteral

Overview

GSI-XII (Z-Ile-Leu-CHO) is a cell-permeable, potent, and reversible inhibitor of gamma-secretase. It is primarily utilized as a research tool to investigate the Notch signaling pathway, as gamma-secretase is the enzyme complex responsible for the intramembrane proteolytic release of the Notch intracellular domain (NICD). By blocking this cleavage, GSI-XII prevents Notch-mediated gene transcription. In oncology research, particularly in multiple myeloma, GSI-XII has been used to study the mechanisms of chemoresistance and the role of the bone marrow microenvironment in tumor cell survival. It was historically developed and distributed as a laboratory reagent by Calbiochem (a brand of Merck KGaA).

Other names: gamma-secretase inhibitor XIIZ-Ile-Leu-aldehyde

Targets

GSEC (Gamma-Secretase Complex)

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