DBZ

DBZ is a diazepine inhibitor of γ-secretase, which cleaves transmembrane proteins including Notch, amyloid precursor protein. DBZ blocks the cleavage of Notch into its active signalling effector, Notch intracellular domain, with an IC₅₀ of 1. 7 nM. Enables reprogramming of human keratinocytes to induced pluripotent stem cells in the absence of oncogenic reprogramming factors KLF4 and c-MYC. Induces intestinal cell apoptosis & goblet cell metaplasia in rats; attenuates the reduction of paneth cells and goblet cells caused by tuberous sclerosis 2. Improves glucose homeostasis and mediates a metabolic shift toward the utilization of fat as the energy source in mice. Induces differentiation of intestinal adenomas in Apc(Min) transgenic mice. Decreases the production of inflammatory cytokines by alloreactive T cells after bone marrow transplantation in mice, reducing the severity of graft-versus-host disease.