Talabostat mesylate, Pyroptosis inducer; Inflammasome activator (TBI4005)

Description

Product Details

Formal Name: ((2R)-1-((2S)-2-Amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid methanesulfonate

Alternate Names: Val-boroPro; PT-100

Molecular Formula: C₉H₁₉BN₂O₃·CH₃SO₃H

Formula Weight: 310.18

CAS Number: 1510080-09-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Pyroptosis inducer; Inflammasome activator

Functions

Talabostat mesylate 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). 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. It mediates tumor regression by accelerating the expansion of tumor-specific T cells. 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. Pyroptosis induction by DPP8/9 inhibition has been shown to be caused by activation of the inflammasome sensor protein Nlrp1b.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.