Talabostat mesylate

- Overview
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    Background
    
    IC50: 1 nM
    Talabostat mesilate (PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases for DPP4, including tumor-associated fibroblast activation protein- (FAP).
    Fibroblast activation protein- (FAP), as an integral membrane serine protease and member of the post-prolyl peptidase family, closely related to dipeptidyl peptidase IV (DPPIV) and displays a DPPIV-like fold with the characteristic /-hydrolase and eightbladed -propeller domains [1].
    In vitro: By the cleavage of N-terminal Xaa-Pro or Xaa-Ala residues, talabostat blocks dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in inducing the production of cytokine and chemokine (besides specific T-cell immunity and T-cell-dependent activity). This agent may also induce the production of colony stimulating factors, for instance, granulocyte colony stimulating factor (G-CSF), resulting in the inducement of hematopoiesis. Dipeptidyl peptidases are referred to the activation of polypeptide hormones and chemokines.
    Talabostat slightly lowered the growth rates of the FAP-expressing tumors but because PT-630 and LAF-237 did not, the growth blockade was likely not related to inhibit FAP or the related post-prolyl peptidase dipeptidyl peptidase IV.[1]
    In vivo: So far, no study in vivo has been conducted.
    Clinical trial: Clinical study has been conducted.
- Properties
  - CAS Number
    
    150080-09-4
    
    Molecular Formula
    
    C10H23BN2O6S
    
    Molecular Weight
    
    310.18
    
    Appearance
    
    A solid
    
    Purity
    
    99.87%
    
    Solubility
    
    ≥11.45 mg/mL in DMSO; ≥31 mg/mL in H2O; ≥8.2 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Andreas Linder, Stefan Bauernfried, et al. "CARD8 inflammasome activation triggers pyroptosis in human T cells." EMBO J 2020 Aug 25;e105071. PMID:32840892
    2. Chen M, Lei X, et al. "Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents." J Clin Invest. 2017 Oct 2;127(10):3689-3701. PMID:28846068
    3. Feng X, Wang Q, et al. "A synthetic urinary probe-coated nanoparticles sensitive to fibroblast activation protein α for solid tumor diagnosis." Int J Nanomedicine. 2017 Jul 27;12:5359-5372. PMID:28794628

Talabostat mesylate

Background

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