CAT # | Khoom npe | Kev piav qhia |
PAB 100573 | PF-05175157 | PF-05175157 yog ib qho muaj zog thiab xaiv inhibitor ntawm ob qho tib si acetyl-CoA carboxylase isoform ACC1 nyob hauv daim siab thiab cov ntaub so ntswg adipose thiab isoform ACC2 tseem ceeb hauv cov pob txha thiab lub plawv, nrog IC50 qhov tseem ceeb ntawm 27 nM thiab 33 nM, raws li. ACC inihibitors inhibit de novo lipogenesis thiab nce β-oxidation ntawm cov saw ntev fatty acids uas muaj peev xwm rau kev kho mob ntawm hom 2 mob ntshav qab zib, hepatic steatosis, thiab mob qog noj ntshav. |
PIB 100572 | NWS-646 | ND-646 yog-ib qho allosteric inhibitor ntawm ACC enzymes ACC1 thiab ACC2 uas tiv thaiv ACC subunit dimerization-kom suppress fatty acid synthesis hauv vitro thiab hauv vivo. Kev kho mob ntev ND-646 ntawm xenograft thiab genetic engineered nas qauv ntawm NSCLC inhibited qog loj hlob. Thaum siv los ua ib tus neeg sawv cev lossis ua ke nrog cov tshuaj carboplatin tus qauv, ND-646 tau ua rau muaj kev cuam tshuam lub ntsws loj hlob hauv Kras; Trp53-/- (tseem hu ua KRAS p53) thiab Kras; Stk11-/- ( tseem hu ua KRAS Lkb1) nas qauv ntawm NSCLC. ND-646 tau txhim kho kev ua tau zoo thaum ua ke nrog carboplatin, ib feem ntawm cov tshuaj kws khomob siv los kho tib neeg NSCLC. |
PIB 100571 | Qauv TSIS MUAJ: CP-640186 | CP-640186 yog ib qho muaj zog inhibitor ntawm mammalian ACCs thiab tuaj yeem txo lub cev hnyav thiab txhim kho insulin rhiab heev hauv cov tsiaj sim. CP-640186 tsis ntev los no tau pom tias yog ib qho muaj zog inhibitor ntawm isoforms ntawm mammalian ACCs nrog IC50 qhov tseem ceeb ntawm 55 nM. Qhov no yog tam sim no tsuas yog tshaj tawm muaj zog inhibitor ntawm mammalian ACCs. Hauv cov kab lis kev cai ntawm tes thiab hauv cov qauv tsiaj, CP-640186 tuaj yeem txo cov ntaub so ntswg malonyl-CoA qib, inhibit fatty acid biosynthesis, thiab txhawb cov fatty acid oxidation. Qhov tseem ceeb tshaj plaws, CP-640186 tuaj yeem txo cov rog hauv lub cev thiab lub cev hnyav, thiab txhim kho cov tshuaj insulin, ua kom pom tseeb ACCs raws li lub hom phiaj rau kev tiv thaiv kev rog thiab tshuaj tiv thaiv kab mob ntshav qab zib. |
PEB 1592 | NWS-630 | ND-630 yog ib qho acetyl-CoA carboxylase (ACC) inhibitor; inhibits tib neeg ACC1 thiab ACC2 nrog IC50 qhov tseem ceeb ntawm 2.1 thiab 6.1 nM, feem. |