Talabostat (mesylate)

Talabostat (mesylate)

• Product Name Alternative: Val-boroPro (mesylate); PT100 (mesylate)
• CAS Number: 150080-09-4
• UNSPSC Description: Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 Ki = 0.18 nM) and the 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].
• Target Antigen: Dipeptidyl Peptidase
• Type: Reference compound
• Related Pathways: Metabolic Enzyme/Protease
• Field of Research: Cancer; Inflammation/Immunology
• Assay Protocol: https://www.medchemexpress.com/Talabostat-mesylate.html
• Purity: 98.35
• Solubility: DMSO : ≥ 40 mg/mL|H2O : 250 mg/mL (ultrasonic)
• Smiles: CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O.CS(=O)(O)=O
• Molecular Weight: 310.18
• 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.Adv Sci (Weinh). 2023 Jun 21;e2300881.|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 Mar 20.|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. 2024 Oct 5:S2090-1232(24)00433-8.|J Allergy Clin Immunol. 2021 Jun;147(6):2134-2145.e20.|J Biol Chem. 2018 Dec 7;293(49):18864-18878. |J Diabetes Investig. 2021 Sep 8.|J Exp Med. 2022 Oct 3;219(10):e20212117.|Nat Commun. 2019 May 7;10(1):2091.|Obesity. 2020 Dec 20.|Proc Natl Acad Sci U S A. 2023 Jan 31;120(5):e2213777120.|Research Square Preprint. 2024 Apr 18.|SSRN. 2020 Jul.|Ann Surg Oncol. 2020 Oct;27(11):4337-4347.|bioRxiv. 2023 Jan 17.|bioRxiv. 2023 Jun 25.|bioRxiv. January 25, 2022.|Cells. 2023 Apr 6, 12(7), 1100.|CNS Neurosci Ther. 2022 Nov 15.|Curr Protoc Immunol. 2020 Dec;131(1):e107.|Int Immunopharmacol. 2023 May 12;120:110291.|Int J Biol Sci. 2023; 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.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Phase 3