| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100573 | PF-05175157 | I-PF-05175157 iyisivimbeli esinamandla nesikhethayo sakho kokubili i-acetyl-CoA carboxylase isoform ACC1 etholakala ikakhulukazi esibindini nasezicubu ze-adipose kanye ne-isoform ACC2 ebusayo kumisipha yamathambo nenhliziyo, ngamavelu e-IC50 angu-27 nM no-33 nM, ngokulandelana. I-ACC inhibitors inhibit de novo lipogenesis futhi andise i-β-oxidation yamafutha amaketanga amade anamandla okwelapha uhlobo lwesifo sikashukela sohlobo 2, i-hepatic steatosis, nomdlavuza. |
| I-CPD100572 | ND-646 | I-ND-646 iyi-allosteric inhibitor ye-ACC enzymes i-ACC1 ne-ACC2 evimbela i-ACC subunit dimerization-ukucindezela ukuhlanganiswa kwe-fatty acid in vitro kanye ne-vivo. Ukwelashwa okungapheli kwe-ND-646 ye-xenograft kanye namamodeli egundane enziwe ngofuzo we-NSCLC avimbele ukukhula kwesimila. Lapho isetshenziswa njenge-ejenti eyodwa noma ihlanganiswe nesidakamizwa esisezingeni lokunakekela i-carboplatin, i-ND-646 icindezele ngokuphawulekayo ukukhula kwesimila samaphaphu e-Kras;Trp53-/- (eyaziwa nangokuthi i-KRAS p53) kanye ne-Kras;Stk11-/- ( eyaziwa nangokuthi i-KRAS Lkb1) amamodeli wamagundane we-NSCLC. I-ND-646 ibe nokusebenza okuthuthukisiwe uma ihlanganiswa ne-carboplatin, ingxenye evamile yemithi yokwelapha i-chemotherapeutic esetshenziselwa ukwelapha i-NSCLC yomuntu. |
| I-CPD100571 | I-CP-640186 | I-CP-640186 iyisivimbeli esinamandla sama-mammalian ACCs futhi ingehlisa isisindo somzimba futhi ithuthukise ukuzwela kwe-insulin ezilwaneni ezihlolayo. I-CP-640186 isanda kuboniswa iyisivimbeli esinamandla sama-isoforms ama-mammalian ACC anamanani e-IC50 acishe abe ngu-55 nM. Lokhu okwamanje ukuphela kwe-inhibitor enamandla ebikwayo yama-mammalian ACCs. Emasikweni amaseli kanye nasemamodelini ezilwane, i-CP-640186 inganciphisa amazinga e-malonyl-CoA ezicubu, ivimbele i-fatty acid biosynthesis, futhi ivuse i-oxidation ye-fatty acid. Okubaluleke kakhulu, i-CP-640186 inganciphisa isisindo somzimba kanye nesisindo somzimba, futhi ithuthukise ukuzwela kwe-insulin, iqinisekise ama-ACC njengemigomo yezidakamizwa ze-antiobesity kanye ne-antidiabetes. |
| I-CPD1592 | ND-630 | I-ND-630 iyi-acetyl-CoA carboxylase (ACC) inhibitor; ivimbela i-ACC1 yomuntu ne-ACC2 enamanani e-IC50 angu-2.1 no-6.1 nM, ngokulandelanayo. |
