Cell-permeable factor XIIIa and transglutaminase 2 irreversible inhibitor that targets active site Cys for acetonylation with little GSH inhibitory potency.
R283 (NTU283; Rob283) is a cell-permeable 2-[(2-oxopropyl)thio] imidazolium derivative that acts as an irreversible inhibitor against factor XIIIa (FXIIIa) and transglutaminase 2 (TG2, TGase II) by targeting FXIIIa and TG2 active site cysteine (Cys) for acetonylation in a selective manner with little glutathione (GSH) inhibitory potency (app 2nd order rate const = 23000/M/s, 19000/M/s, 0.12/M/s, respectively). A useful tool for investigating TG2-mediated cellular functions (typical conc. range: 25-500 μM).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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In celiac disease (CD), transglutaminase type II (TG2) has 2 fundamental roles: (1) as the autoantigen recognized by highly specific autoantibodies and (2) the modifier of pathogenic gliadin T-cell epitopes. It follows that inhibition of TG2 might represent an attractive
The British journal of dermatology, 156(2), 247-257 (2007-01-17)
The transglutaminase (TG) family consists of eight distinct isoforms. TG types 1, 3 and 5 play a major role in normal skin development, with TG2 also being elevated during dermal wounding. TG1, 3 and 5 are responsible for the cross-linking
Deposition of amyloid-beta (Aβ) peptides has been shown to induce the release of inflammatory factors by activated microglia and brain infiltrating monocytes/macrophages. Interestingly, the enzyme transglutaminase 2 (TG2) has been shown to play a key role in neuroinflammation and regulation
We previously reported the importance of induced nuclear transglutaminase (TG) 2 activity, which results in hepatic cell death, in ethanol-induced liver injury. Here, we show that co-incubation of either human hepatic cells or mouse primary hepatocytes derived from wild-type but
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