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Talabostat

Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 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].

Product Specifications

CAS Number

[149682-77-9]

Product Name Alternative

Val-boroPro; PT100

UNSPSC

12352005

Target

Dipeptidyl Peptidase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Talabostat.html

Solubility

DMSO : ≥ 40 mg/mL

Smiles

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

Molecular Formula

C9H19BN2O3

Molecular Weight

214.07

References & Citations

[1]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.|[2]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.|[3]Talabostat|[4]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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

DPP-4

Citation 01

Ann Surg Oncol. 2020 Oct;27 (11) :4337-4347.|bioRxiv. 2023 Jan 17.|bioRxiv. 2023 Jun 25.|bioRxiv. 2025 Aug 16.|bioRxiv. January 25, 2022.|Cells. 2023 Apr 6;12 (7) :1100.|CNS Neurosci Ther. 2023 Mar;29 (3) :878-892.|Curr Protoc Immunol. 2020 Dec;131 (1) :e107.|Int Immunopharmacol. 2023 Jul:120:110291.|Int J Biol Sci. 2023 Jan 1;19 (2) :465-483.|Iran J Allergy Asthma Immunol. 2021 Mar 17.|J Biol Chem. 2018 Dec 7;293 (49) :18864-18878. |J Immunol. 2020 Sep 15;205 (6) :1653-1663.|Proc Natl Acad Sci U S A. 2019 Sep 17;116 (38) :19055-19063. |Sci Signal. 2023 Jan 17;16 (768) :eabh1083.|Science. 2020 Dec 4;370 (6521) :eaay2002.|Adv Sci (Weinh) . 2023 Aug;10 (24) :e2300881.|Adv Sci (Weinh) . 2025 Jan 17:e2409147.|Anal Chem. 2016 Aug 16;88 (16) :8309-14. |Biomolecules. 2024 Mar 25;14 (4) :391.|bioRxiv. 2023 Mar 19.|bioRxiv. 2023 Nov 4.|Cancer Commun (Lond) . 2024 May;44 (5) :554-575.|Cancer Res. 2016 Jul 15;76 (14) :4124-35. |Cell Rep. 2021 Oct 26;37 (4) :109904.|Cell. 2023 May 11;186 (10) :2144-2159.e22.|Cell. 2024 Feb 29;187 (5) :1223-1237.e16.|J Adv Res. 2025 Aug:74:225-236.|J Allergy Clin Immunol. 2021 Jun;147 (6) :2134-2145.e20.|J Biol Chem. 2018 Dec 7;293 (49) :18864-18878. |J Diabetes Investig. 2022 Jan;13 (1) :22-33.|J Exp Med. 2022 Oct 3;219 (10) :e20212117.|J Exp Med. 2025 Nov 3;222 (11) :e20242403.|Nat Commun. 2019 May 7;10 (1) :2091.|Neurosci Bull. 2025 Jan;41 (1) :16-32.|NPJ Dement. 2025;1 (1) :3.|Obesity. 2021 Feb;29 (2) :327-336.|Proc Natl Acad Sci U S A. 2023 Jan 31;120 (5) :e2213777120.|Research Square Preprint. 2024 Apr 18.|SSRN. 2020 Jul.|SSRN. 2025 Jan 28.

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