2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. 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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Talabostat Related Antibodies

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Talabostat

WB

    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.

    View All Dipeptidyl Peptidase Isoform Specific Products:

    View All Isoforms
    DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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    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

    DPP-4

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    0.066 μM
    Compound: 1, PT-100
    Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
    Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
    		[PMID: 24617858]
    HEK293 IC50
    0.066 μM
    Compound: 1, PT-100, Val-boroPro
    Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
    Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
    		[PMID: 22525314]
    HEK293 IC50
    0.07 μM
    Compound: 1, PT- 100, Talabostat
    Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
    Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
    		[PMID: 24900696]
    HEK-293T IC50
    6.8 μM
    Compound: 1, Val-boroPro
    Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
    Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
    		[PMID: 18783201]
    U-87MG ATCC IC50
    0.224 μM
    Compound: Talabostat
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
    		[PMID: 32527554]
    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.

    Talabostat Related Antibodies
    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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    Talabostat Related Classifications

    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.

    Keywords:

    Talabostat149682-77-9Val-boroPro PT100PT100PT 100PT-100Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

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