Talabostat (PT-100)

For research use only.

Catalog No.S8455 Synonyms: Val-boroPro

1 publication

Talabostat (PT-100) Chemical Structure

Molecular Weight(MW): 310.18

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.

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Selleck's Talabostat (PT-100) has been cited by 1 publication

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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)
DPP8 [1]
(Cell-free assay)
DPP9 [1]
(Cell-free assay)
QPP [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].

Assay
Methods Test Index PMID
Western blot
pro-IL-1β; 

PubMed: 27820798     


The effects of Val-boroPro (2 μM, 24 h) on IL-1β expression and secretion in THP-1 macrophages as determined by immunoblotting

27820798
Growth inhibition assay
Cell viability; 

PubMed: 29967349     


Dose response of cell viability of sensitive (b) and resistant (c) cell lines to treatment with Val-boroPro (24 h for MV4;11 and RS4;11 cells, 48 h for all others) relative to DMSO.

29967349
ELISA
IL-1β; 

PubMed: 27820798     


The effects of Val-boroPro (2 μM, 24 h) on IL-1β expression and secretion in THP-1 macrophages as determined by ELISA

27820798
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

Cell Research:

[4]

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  • Cell lines: THP-1 macrophages
  • Concentrations: 0.1, 1, 10 μM
  • Incubation Time: 24 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[3]

- Collapse
  • Animal Models: C57BL/6 female mice
  • Dosages: 20 µg
  • Administration: by gavage
    (Only for Reference)

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)

* 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.

Chemical Information

Molecular Weight 310.18
Formula

C10H23BN2O6S

CAS No. 150080-09-4
Storage powder
in solvent
Synonyms Val-boroPro
Smiles CC(C)C(N)C(=O)N1CCCC1B(O)O.C[S](O)(=O)=O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID