Talabostat mesylate |CAS:150080-09-4 Probechem Biochemicals

Chemical Structure : Talabostat mesylate

CAS No.: 150080-09-4

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Talabostat mesylate (PT-100;ValboroPro;Val-boroPro;PT100;PT 100)

货号: PC-43412Not 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.

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25 mg	￥2680	In stock
100 mg	￥5680	In stock
500 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	310.1754
分子式	C10H23BN2O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 40 mg/mL
Chemical Name/SMILES	Boronic acid, B-[(2R)-1-[(2S)-2-amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]-, methanesulfonate (1:1)

参考文献

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 mesylate (PT-100;ValboroPro;Val-boroPro;PT100;PT 100)

生物&药学活性

物理化学性质&存储条件

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Talabostat mesylate (PT-100;ValboroPro;Val-boroPro;PT100;PT 100)

生物&药学活性

物理化学性质&存储条件

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