| CAT # | Igama lemveliso | Inkcazo |
| CPD100573 | PF-05175157 | I-PF-05175157 yi-inhibitor enamandla kwaye ekhethiweyo yazo zombini i-acetyl-CoA carboxylase isoform ACC1 efumaneka ngokukodwa kwisibindi kunye nezicubu ze-adipose kunye ne-isoform ye-ACC2 eyongameleyo kwi-skeletal and heart muscle, kunye ne-IC50 ixabiso le-27 nM kunye ne-33 nM, ngokulandelanayo. I-ACC inhibitors inhibit de novo lipogenesis kunye nokwandisa i-β-oxidation ye-long-chain fatty acids enokubakho kunyango lwe-2 yeswekile, i-hepatic steatosis, kunye nomhlaza. |
| CPD100572 | ND-646 | I-ND-646 yi-allosteric inhibitor ye-ACC enzymes i-ACC1 kunye ne-ACC2 ethintela i-ACC subunit dimerization-ukucinezela i-fatty acid synthesis in vitro kunye ne-vivo. Unyango olungapheliyo lwe-ND-646 ye-xenograft kunye neemodeli zemouse ezenziwe ngofuzo ze-NSCLC zithintele ukukhula kwethumba. Xa ilawulwa njenge-arhente enye okanye idityaniswe ne-carboplatin esemgangathweni yeziyobisi, i-ND-646 icinezele ngokuphawulekayo ukukhula kwethumba emiphunga kwi-Kras; Trp53-/- (ekwaziwa ngokuba yi-KRAS p53) kunye ne-Kras; Ikwabizwa ngokuba yi-KRAS Lkb1) imifuziselo yempuku ye-NSCLC. I-ND-646 iye yaphucula ukusebenza kakuhle xa idityaniswe ne-carboplatin, icandelo eliqhelekileyo lerejimeni ze-chemotherapeutic ezisetyenziselwa ukunyanga i-NSCLC yabantu. |
| CPD100571 | CP-640186 | I-CP-640186 yi-inhibitor enamandla ye-mammalian ACCs kwaye inokunciphisa ubunzima bomzimba kunye nokuphucula ukuvakalelwa kwe-insulin kwizilwanyana zokuvavanya. I-CP-640186 kutshanje ibonakaliswe njenge-inhibitor enamandla ye-isoforms ye-mammalian ACCs kunye nexabiso le-IC50 malunga ne-55 nM. Oku ngoku kuphela kwe-inhibitor enamandla exeliweyo yee-ACCs ezincancisayo. Kwiinkcubeko zeeseli kunye nakwiimodeli zezilwanyana, i-CP-640186 inokunciphisa amanqanaba e-malonyl-CoA e-tissue, inhibit i-fatty acid biosynthesis, kwaye ivuselele i-acid acid oxidation. Okubaluleke kakhulu, i-CP-640186 inokunciphisa ubunzima bomzimba kunye nobunzima bomzimba, kwaye iphucule i-insulin sensitivity, iqinisekisa ii-ACC njengeethagethi ze-antiobesity kunye neziyobisi ze-antidiabetes. |
| CPD1592 | ND-630 | I-ND-630 i-acetyl-CoA carboxylase (ACC) inhibitor; inqanda i-ACC1 yomntu kunye ne-ACC2 enexabiso le-IC50 le-2.1 kunye ne-6.1 nM, ngokulandelelanayo. |
