A non-selective inhibitor of dipeptidyl peptidases
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Talabostat (mesylate)

Item No. 29007

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlEthanol: 1 mg/mlPBS (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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $65

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    25 mg

    $149

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    50 mg

    $270

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    Cayman Chemical
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    Product Description

    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).1 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-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lankas, G.R., Leiting, B., Roy, R.S., et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: Potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes 54(10), 2988-2994 (2005).

    2. Adams, S., Miller, G.T., Jesson, M.I., 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. 64(15), 5471-5480 (2004).