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Talabostat

(Synonyms: Val-boroPro; PT100)
43 Cited Publications
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Based on 43 publication(s) in Google Scholar

Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Talabostat mesylate) that retains the same biological activity.

For research use only. We do not sell to patients.

  • Purity : 95.20%
  • CAS No.: 149682-77-9
  • Formula: C9H19BN2O3
  • Molecular Weight:214.07
  • Storage:
    Powder   -20°C, 3 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • Talabostat Chemical Structure
    Talabostat Chemical Structure
  • Experimental Validation Results for Talabostat
  • Experimental Validation Results for Talabostat
  • Experimental Validation Results for Talabostat
  • Experimental Validation Results for Talabostat
  • Experimental Validation Results for Talabostat
  • Experimental Validation Results for Talabostat
CAS No.: 149682-77-9
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Find Your Local Distributor Your local distributor: Hycultec GmbHHycultec
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  • In Vivo Efficacy Study
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  • Talabostat Chemical Structure
    Talabostat Chemical Structure
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    Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]

    Customer Validation
     Activation of CARD8 inflammasome by HIV-1 in THP-1 cells. CARD8-KO THP-1 cells expressing wild-type or mutant CARD8 were exposed to HIV reporter virus NL4-3-ΔEnv-EGFP pseudotyped with the VSVG envelope for six hours before LDH. Talabostat mesylate (VbP, 5 μM) was used as a positive control, as it induces cell death and IL-1β secretion.

  • 1/16

    Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]

    Customer Validation
     Talabostat mesylate (20 µg/mouse; i.g.; once daily for 21 days) effectively inhibited tumor growth in BALB/c mice bearing 4T1 cells.

  • 1/16

    Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]

    Customer Validation
     LDH release and IL-1b secretion by ELISA in cell-free supernatants of N/TERT-1 stably expressing mCitrine (control) or bat/human ASC2-mCitrine, treated with Talabostat mesylate (2-200 μM) for 24 h.

  • 1/16

    Talabostat purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]

    Customer Validation
     Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.

  • 1/16

    Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]

    Customer Validation
     RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Cleaved caspase-3 in the cells was detected by Western blotting. The results indicate that Talabostat mesylate can activate caspase‑3 in Gsdmd‑knockout cells.

  • 1/16

    Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]

    Customer Validation
     RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Microscopic images of the cells. The results showed that Talabostat mesylate induced apoptotic morphological changes in Gsdmd‑knockout cells.

  • Talabostat