Home>>Signaling Pathways>> Proteases>> Dipeptidyl Peptidase>>Talabostat mesylate

Talabostat mesylate (Synonyms: Val-boro-Pro)

Catalog No.GC10018

Talabostat (PT100) is an inhibitor of the dipeptidyl peptidase (DPP) family, with IC50 values of <4 nM for DPP-IV, 4 nM for DPP8, 11 nM for DPP9, 310 nM for QPP, 560 nM for FAP, and 390 nM for PEP. It exhibits anti-tumor activity and stimulatory effects on hematopoiesis.

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Talabostat mesylate Chemical Structure

Cas No.: 150080-09-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$73.00
In stock
10mg
$126.00
In stock
50mg
$288.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

THP-1 cells, RAW 264.7 and J774 cells

Preparation method

THP-1 cells were differentiated in 10 cm dishes in complete medium with 50 ng/mL PMA for 3 d. RAW 264.7 and J774 cells were plated at 3 × 106 cells per 10 cm plate in complete medium and incubated overnight. The cells were washed with 2 × 5 mL PBS before the addition of 10 mL of serum free media. Cells were then treated with Talabostat (PT100) (2 μM) or LPS (10 μg/mL) for 24 h.

Reaction Conditions

2 μM; 24 h

Applications

Talabostat (PT100) induces an active form of pro-caspase-1 that can sufficiently cleave a substrate (or substrates) that mediates pyroptosis, but that does not efficiently cleave IL-1β or the tetrapeptide Ac-WEHD-AFC.

Animal experiment [2]:

Animal models

BALB/c, C56BL/6, DBA/2, and BALB/cnu/nu mice

Preparation method

Tumor-inoculated mice were given varying doses (5–40 μg) of Talabostat(PT100) or saline vehicle by oral gavage, twice daily at ∼8h intervals. The time of tumor inoculation was defined as day 0, and PT-100 treatment was started on either day 2 or day 7 and continued daily.

Dosage form

5–40 μg twice daily at ∼8h intervals;p.o.

Applications

Treatment with Talabostat(PT100) was found to significantly inhibit the additional growth of B16-F10, WEHI 164 and EL 4 tumor cells in mice.

References:

[1] Okondo M C , Johnson D C , Sridharan R ,et al.DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis[J].Nature Chemical Biology, 2017 Jan; 13(1): 46–53.

[2] Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. 

Background

Talabostat (PT100) is an orally active and non-selective inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50= 560 nM), inhibiting DPP 8/9 (IC50= 4/11 nM; Ki = 1.5/0.76 nM), prolyl endopeptidase (QPP) (IC50= 310 nM), DPP2, and other DASH family enzymes[1]. Due to its inhibitory action on these proteases, the mechanism of action of Talabostat (PT100) involves the inhibition of protease activity, thereby affecting the tumor microenvironment, immune cell activity, and inflammatory responses[2]. Talabostat (PT100) is also known to stimulate hematopoiesis.

In vitro, Talabostat (PT100) at concentrations ranging from 30 pg/ml to 30 μg/ml when added to the culture medium, can induce tumor regression and rejection in WEHI 164 fibrosarcoma and EL 4 and A20/2 J lymphoma models[1]. Talabostat (PT100) (2μM, 24h) can induce the active form of caspase-1, which can efficiently cleave substrates mediating pyroptosis but not effectively cleave IL-1β or the tetrapeptide Ac-WEHD-AFC[4]. In tumors and tumor-draining lymph nodes, Talabostat (PT100) stimulates the transcriptional upregulation of various cytokines such as IL-1β, IL-6, G-CSF, and CXCL1/KC[4].

In vivo, Talabostat (PT100) significantly inhibits the extraneous growth of tumors such as B16-F10, WEHI 164, and EL 4 tumor cells in mice through delayed oral administration (5–40 μg, twice daily, approximately 8 hours apart) [3].

References:

[1] Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13.

[2] Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94.

[3] Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80.

[4] Okondo M C , Johnson D C , Sridharan R ,et al.DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis[J].Nature Chemical Biology, 2017 Jan; 13(1): 46–53.

Chemical Properties

Cas No. 150080-09-4 SDF
Synonyms Val-boro-Pro
Canonical SMILES OS(=O)(C)=O.O=C([C@H](C(C)C)N)N1[C@H](B(O)O)CCC1
Formula C10H23BN2O6S M.Wt 310.18
Solubility ≥ 11.45mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.2239 mL 16.1197 mL 32.2393 mL
5 mM 0.6448 mL 3.2239 mL 6.4479 mL
10 mM 0.3224 mL 1.612 mL 3.2239 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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