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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.

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  • Reinheit : 95.20%
  • CAS. Nr.: 149682-77-9
  • Formel: C9H19BN2O3
  • Molecular Weight:214.07
  • Speicherung:
    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. Nr.: 149682-77-9
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  • In Vivo Efficacy Study
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  • Talabostat Chemical Structure
    Talabostat Chemical Structure
    1/16
  • 1/16

    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