Cas No.: | 149682-77-9 |
Chemical Name: | Boronic acid, B-[(2R)-1-[(2S)-2-amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]- |
Synonyms: | PT-100;ValboroPro;Val-boroPro;PT100;PT 100 |
SMILES: | CC(C)C(N)C(=O)N1C(B(O)O)CCC1 |
Formula: | C9H19BN2O3 |
M.Wt: | 214.072 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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; induces powerful anti-tumor immune responses in syngeneic cancer models; 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; activates the inflammasome sensor protein Nlrp1b, which in turn activates pro-caspase-1 to mediate pyroptosis. Solid Tumors Phase 1 Clinical |