Talabostat (mesylate)

Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP, IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively). It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs, IC50 = ~10 nM). Talabostat (5 µg twice per day) increases expression of a variety of cytokines, including those encoding IL-1beta, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model. It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.Formal Name: B-[(2R)-1-[(2S)-2-amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]-boronic acid, methanesulfonate. CAS Number: 150080-09-4. Synonyms: Val-boro-Pro. Molecular Formula: C9H19BN2O3 . CH3SO3H. Formula Weight: 310.2. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: CC(C)[C@H](N)C(N1CCC[C@H]1B(O)O)=O.CS(=O)(O)=O. InChi Code: InChI=1S/C9H19BN2O3.CH4O3S/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15,1-5(2,3)4/h6-8,14-15H,3-5,11H2,1-2H3,1H3,(H,2,3,4)/t7-,8-,/m0./s1. InChi Key: OXYYOEIGQRXGPI-WSZWBAFRSA-N.