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Talabostat mesylate

Catalog #: 3719
5 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3719/50
3719/10
Talabostat mesylate | CAS No. 150080-09-4 | Inflammasomes Activators
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Description: Potent DPP IV inhibitor; activates NLRP1b inflammasome
Alternative Names: Val-boroPro, BXCL 701

Chemical Name: B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate

Purity: ≥98%

Product Details
Citations (5)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Talabostat mesylate is a potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.

Technical Data

M.Wt:
310.18
Formula:
C9H19BN2O3.CH3SO3H
Solubility:
Soluble to 100 mM in water and to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
150080-09-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis.
    Okondo MC, Johnson DC, Sridharan R et al.
    Nat. Chem. Biol.
  2. Inhibition of Dpp8/9 activates the Nlrp1b inflammasome.
    Okondo et al.
    Cell Chem.Biol., 2018;25:262

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Citations for Talabostat mesylate

The citations listed below are publications that use Tocris products. Selected citations for Talabostat mesylate include:

5 Citations: Showing 1 - 5

  1. Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation.
    Authors: Orth-He Et al.
    Cell Rep  2023;42:111965
  2. A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome.
    Authors: Daniel A Et al.
    J Biol Chem  2022;298:102032
  3. PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index.
    Authors: Massimiliano Et al.
    Mol Cancer Ther  2022;21:568-581
  4. M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome.
    Authors: Justin R Et al.
    Nat Chem Biol  2022;18:565-574
  5. The half-life of the bone-derived hormone osteocalcin is regulated through O-glycosylation in mice, but not in humans.
    Authors: Henrik Et al.
    Elife  2020;9

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