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Talabostat mesylate | Pyroptosis inducer / Inflammasome activator

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 cell signaling supplier, chemical structure of Talabostat mesylate | Pyroptosis inducer | CAS 150080-09-4

Catalog#  10-4005-0010

$70.00
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CAS:
150080-09-4
Catalog Number:
10-4005
Activity:
Pyroptosis inducer / Inflammasome activator
Chemical Name:
((2R)-1-((2S)-2-Amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid methanesulfonate
Alternate Names:
Val-boroPro; PT-100
Molecular Weight:
310.18
Molecular Formula:
C9H19BN2O3 • CH3SO3H
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
97% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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