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 1
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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 1
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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