Chemical Name: B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate
Biological ActivityTalabostat mesylate is a potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis.
Okondo MC, Johnson DC, Sridharan R et al.
Nat. Chem. Biol.
Inhibition of Dpp8/9 activates the Nlrp1b inflammasome.
Okondo et al.
Cell Chem.Biol., 2018;25:262
Citation for Talabostat mesylate
The citations listed below are publications that use Tocris products. Selected citations for Talabostat mesylate include:
1 Citation: Showing 1 - 1
Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation.
Authors: Orth-He Et al.
Cell Rep 2023;
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