Talabostat (PT-100, Val-boroPro) | DPP4 inhibitor

Chemical Structure : Talabostat

CAS No.: 149682-77-9

Talabostat (PT-100, ValboroPro, Val-boroPro, PT100)

Catalog No.: PC-50014Not For Human Use, Lab Use Only.

Talabostat (PT-100, Val-boroPro) is a potent, nonselective, orally available inhibitor of post-proline cleaving serine proteases with Ki of 0.18 nM for DPP4, also potently inhibits DPP8/9 (IC50=1.5/0.76 nM), FAP, DPP2 and some other DASH family enzymes.

Packing	Price	Stock
5 mg	$88	In stock
10 mg	$128	In stock
25 mg	$218	In stock
50 mg	$358	In stock
100 mg		Get quote

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Biological Activity

Talabostat (PT-100, Val-boroPro) is a potent, nonselective, orally available inhibitor of post-proline cleaving serine proteases with Ki of 0.18 nM for DPP4, also potently inhibits DPP8/9 (IC50=1.5/0.76 nM), FAP, DPP2 and some other DASH family enzymes.

Talabostat induces powerful anti-tumor immune responses in syngeneic cancer models.

Talabostat shows the inhibition of the highly related cytosolic serine proteases Dpp8 and Dpp9 (Dpp8/9) by Val-boroPro was recently demonstrated to trigger an immunostimulatory form of programmed cell death known as pyroptosis selectively in monocytes and macrophages.

Talabostat activates the inflammasome sensor protein Nlrp1b, which in turn activates pro-caspase-1 to mediate pyroptosis.

Physicochemical Properties

M.Wt	214.072
Formula	C9H19BN2O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Boronic acid, B-[(2R)-1-[(2S)-2-amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]-

References

1. Connolly BA, et al. J Med Chem. 2008 Oct 9;51(19):6005-13.

2. Cristillo AD, et al. Biochem Biophys Res Commun. 2008 May 23;370(1):22-6.

3. Okondo MC, et al. Cell Chem Biol. 2018 Mar 15;25(3):262-267.

4. Okondo MC, et al. Nat Chem Biol. 2017 Jan;13(1):46-53.

Talabostat (PT-100, ValboroPro, Val-boroPro, PT100)

Biological Activity

Physicochemical Properties

References

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