Talabostat mesylate | Pyroptosis inducer / Inflammasome activator
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 10 mg | $60.00 | ||
| 50 mg | $235.00 |
Talabostat mesylate (150080-09-4) is a non-selective inhibitor of the S9 family of serine proteases (IC50’s: DPPIV = <4nM, DPP8 = 4nM, DPP9 = 11nM, QPP = 310nM, FAP = 560nM, PEP = 390nM).1 Toxicity caused by DPP8/9 inhibition observed with non-selective DPPIV inhibitors limits their use as a diabetes treatment. However, Talabostat displays potent antitumor effects dependent on an intact host immune response.2 It mediates tumor regression by accelerating the expansion of tumor-specific T cells.3 Additionally, DPP8/9 inhibition by Talabostat activates the proprotein form of Caspase-1 leading to a proinflammatory form of cell death in monocytes and macrophages – pyroptosis.4 Pyroptosis induction by DPP8/9 inhibition has been shown to be caused by activation of the inflammasome sensor protein NLRP1B.5
References/Citations:
1) Lankas et al. (2005) Dipeptidyl Peptidase IV Inhibition for the Treatment of Type 2 Diabetes; Diabetes 54 2988
2) Adams et al. (2004) PT-100,a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism; Cancer Res. 64 5471
3) Walsh et al. (2013) Val-BoroPro Accelerates T Cell Priming via Modulation of Dendritic Cell Trafficking Resulting in Complete Regression of Established Murine Tumors; PLoS One 8 e58860
4) Okondo et al. (2017) DPP8/9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis; Nat. Chem. Biol. 13 46
5) Okondo et al. (2018) Inhibition of DPP8/9 Activates the Nlrp1b Inflammasome; Cell Chem. Biol. 25 262
NMR (Conforms)
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Product Data Sheet:
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Talabostat mesylate (150080-09-4) is a non-selective inhibitor of the S9 family of serine proteases (IC50’s: DPPIV = <4nM, DPP8 = 4nM, DPP9 = 11nM, QPP = 310nM, FAP = 560nM, PEP = 390nM).1 Toxicity caused by DPP8/9 inhibition observed with non-selective DPPIV inhibitors limits their use as a diabetes treatment. However, Talabostat displays potent antitumor effects dependent on an intact host immune response.2 It mediates tumor regression by accelerating the expansion of tumor-specific T cells.3 Additionally, DPP8/9 inhibition by Talabostat activates the proprotein form of Caspase-1 leading to a proinflammatory form of cell death in monocytes and macrophages – pyroptosis.4 Pyroptosis induction by DPP8/9 inhibition has been shown to be caused by activation of the inflammasome sensor protein NLRP1B.5
References/Citations:
1) Lankas et al. (2005) Dipeptidyl Peptidase IV Inhibition for the Treatment of Type 2 Diabetes; Diabetes 54 2988
2) Adams et al. (2004) PT-100,a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism; Cancer Res. 64 5471
3) Walsh et al. (2013) Val-BoroPro Accelerates T Cell Priming via Modulation of Dendritic Cell Trafficking Resulting in Complete Regression of Established Murine Tumors; PLoS One 8 e58860
4) Okondo et al. (2017) DPP8/9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis; Nat. Chem. Biol. 13 46
5) Okondo et al. (2018) Inhibition of DPP8/9 Activates the Nlrp1b Inflammasome; Cell Chem. Biol. 25 262
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