1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Talabostat

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.

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Talabostat Chemical Structure

Talabostat Chemical Structure

CAS No. : 149682-77-9

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Top Publications Citing Use of Products

31 Publications Citing Use of MCE Talabostat

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

    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.

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    • References

    • Customer Review

    Description

    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[1][2][3].

    IC50 & Target

    IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP)[1]
    Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9)[2]

    In Vitro

    By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity[3].
    Talabostat (Val-boroPro) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Talabostat (Val-boroPro; PT100) can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system.
    In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, Talabostat (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.
    Talabostat (Val-boroPro) treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    214.07

    Formula

    C9H19BN2O3

    CAS No.
    SMILES

    CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 40 mg/mL (186.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.6714 mL 23.3568 mL 46.7137 mL
    5 mM 0.9343 mL 4.6714 mL 9.3427 mL
    View the Complete Stock Solution Preparation Table
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    Purity & Documentation
    References
    Animal Administration
    [4]

    Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.6714 mL 23.3568 mL 46.7137 mL 116.7842 mL
    5 mM 0.9343 mL 4.6714 mL 9.3427 mL 23.3568 mL
    10 mM 0.4671 mL 2.3357 mL 4.6714 mL 11.6784 mL
    15 mM 0.3114 mL 1.5571 mL 3.1142 mL 7.7856 mL
    20 mM 0.2336 mL 1.1678 mL 2.3357 mL 5.8392 mL
    25 mM 0.1869 mL 0.9343 mL 1.8685 mL 4.6714 mL
    30 mM 0.1557 mL 0.7786 mL 1.5571 mL 3.8928 mL
    40 mM 0.1168 mL 0.5839 mL 1.1678 mL 2.9196 mL
    50 mM 0.0934 mL 0.4671 mL 0.9343 mL 2.3357 mL
    60 mM 0.0779 mL 0.3893 mL 0.7786 mL 1.9464 mL
    80 mM 0.0584 mL 0.2920 mL 0.5839 mL 1.4598 mL
    100 mM 0.0467 mL 0.2336 mL 0.4671 mL 1.1678 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Talabostat
    Cat. No.:
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