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TG2-IN-1 is an irreversible inhibitor of transglutaminase 2 (TG2).1 It inhibits guinea pig liver TG2 (IC50 = 4 µM) and inhibits recombinant human Factor XIIIa in a concentration-dependent manner.1,2 TG2-IN-1 (20-500 µM) reduces γ-glutamyl-ε-lysine isopeptide levels, a marker of TG2 activity, in SH-SY5Y cells but, paradoxically, potentiates amyloid-β-induced increases in γ-glutamyl-ε-lysine isopeptide levels in the same cells. It also promotes amyloid-β-induced apoptosis in SH-SY5Y cells.3
WARNING This product is not for human or veterinary use.
1. Synthesis of potent water-
2. Differences in the inhibition of coagulation factor XIII-
3. Inhibition of tissue transglutaminase promotes Aβ-