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Talabostat (mesylate)
$132 – $490
Products Details
Product Description
– Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; 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].
Web ID
– HY-13233A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C10H23BN2O6S
Citations
– Adv Sci (Weinh). 2023 Jun 21;e2300881.|Anal Chem. 2016 Aug 16;88(16):8309-14. |bioRxiv. 2023 Mar 19.|bioRxiv. 2023 Nov 4.|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.|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.|SSRN. 2020 Jul.|Ann Surg Oncol. 2020 Oct;27(11):4337-4347.|bioRxiv. 2023 Jan 17.|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.
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]Talabostat|[3]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.|[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.
CAS Number
– 150080-09-4
Molecular Weight
– 310.18
Compound Purity
– 98.16
SMILES
– CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O.CS(=O)(O)=O
Clinical Information
– Phase 3
Research Area
– Cancer; Inflammation/Immunology
Solubility
– DMSO : ≥ 40 mg/mL|H2O : 250 mg/mL (ultrasonic)
Target
– Dipeptidyl Peptidase
Isoform
– DPP-4
Pathway
– Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
