Talabostat (PT-100)

Catalog No.S8455 Batch:S845501

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Technical Data

Formula

C10H23BN2O6S
Molecular Weight 310.18 CAS No. 150080-09-4
Solubility (25°C)* In vitro DMSO 62 mg/mL (199.88 mM)
Water 62 mg/mL (199.88 mM)
Ethanol 62 mg/mL (199.88 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities.
Targets
DPP-4 [1]
(Cell-free assay)		 DPP-8 [1]
(Cell-free assay)		 DPP-9 [1]
(Cell-free assay)		 DPP-2 [1]
(Cell-free assay)		 PEP [1]
(Cell-free assay)
<4 nM 4 nM 11 nM 310 nM 390 nM
In vitro

In vitro, talabostat upregulates cytokines/chemokines in human bone marrow stromal cells[2]. Talabostat (Val-boroPro) induces monocytes and macrophage cell death. Val-boroPro induced pyroptosis requires caspase-1[4].
In vivo

Talabostat has been shown to produce potent antitumor effects when administered orally in multiple mouse tumor models. Val-boroPro mediates complete tumor regression via a novel mechanism that requires more rapid DC trafficking and subsequent acceleration of T cell priming[3]. In tumor stroma, talabostat can directly target FAP expressed by reactive fibroblasts. Talabostat stimulates innate and adaptive immune responses against tumors involving transcriptional upregulation of cytokines and chemokines[2]. Val-boroPro is known to stimulate the transcriptional upregulation several cytokines, including IL-1β, IL-6, G-CSF, and CXCL1/KC, in both tumors and tumor-draining lymph nodes, and to increase the mouse serum protein levels of several of these cytokines, including G-CSF and CXCL1/KC[4].

Protocol (from reference)

Cell Assay:

[4]
  • Cell lines

    THP-1 macrophages

  • Concentrations

    0.1, 1, 10 μM

  • Incubation Time

    24 h

  • Method

    --
Animal Study:

[3]
  • Animal Models

    C57BL/6 female mice

  • Dosages

    20 µg

  • Administration

    by gavage

Selleck's Talabostat (PT-100) has been cited by 5 publications

Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] PubMed: 36357533
FAP is critical for ovarian cancer cell survival by sustaining NF-κB activation through recruitment of PRKDC in lipid rafts [ Cancer Gene Ther, 2023, 30(4):608-621] PubMed: 36494579
The FAP α -activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway [ Acta Pharm Sin B, 2022, 12(3):1288-1304] PubMed: 35530139
The FAPα-activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway [ Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.08.015] PubMed: None
Inactivation of the cytoprotective major vault protein by caspase-1 and -9 in epithelial cells during apoptosis: caspase-1 and -9 inactivate the major vault protein. [ J Invest Dermatol, 2019, S0022-202X(19)33499-2] PubMed: 31877317

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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