CAT # | Magaca Alaabta | Sharaxaada |
CPD100573 | PF-05175157 | PF-05175157 waa xakameyn awood leh oo la xushay labadaba acetyl-CoA carboxylase isoform ACC1 oo ku yaal beerka iyo unugyada adipose iyo isoform ACC2 oo ku badan lafaha iyo muruqa wadnaha, oo leh IC50 qiimaha 27 nM iyo 33 nM, siday u kala horreeyaan. ACC inihibitors waxay joojisaa de novo lipogenesis waxayna kordhiyaan β-oxidation ee asiidhyada dufanka dheer ee silsiladda dheer leh ee suurtagalka ah daaweynta nooca 2 ee sonkorowga, steatosis cagaarshow, iyo kansarka. |
CPD100572 | ND-646 | ND-646 waa xannibaadaha allosteric ee ACC enzymes ACC1 iyo ACC2 kaas oo ka hortagaya ACC subunit dimerization-si loo xakameeyo isku-dhafka dufanka leh ee vitro iyo in vivo. Daaweynta ND-646 ee daba-dheeraatay ee xenograft iyo moodooyinka jiirka hiddo-wadaha ee NSCLC waxay hakisay koritaanka burada. Marka loo maamulo hal wakiil ama marka lagu daro daawada karboplatin-daryeelka caadiga ah, ND-646 waxay si muuqata u joojisay koritaanka burada sambabada ee Kras; Trp53-/- (oo sidoo kale loo yaqaan KRAS p53) iyo Kras; Stk11-/- ( sidoo kale loo yaqaan KRAS Lkb1) moodooyinka jiirka ee NSCLC. ND-646 ayaa kor u qaaday waxtarka marka lagu daro karboplatin, oo ah qayb caadi ah oo ka mid ah hababka daaweynta kiimiko ee loo isticmaalo daaweynta NSCLC bini'aadamka. |
CPD100571 | CP-640186 | CP-640186 waa horjooge awood leh oo ka mid ah naasleyda ACCs waxayna yareyn kartaa miisaanka jirka waxayna hagaajin kartaa dareenka insulin ee xayawaanka tijaabada. CP-640186 ayaa dhawaan la muujiyay inuu yahay ka hortag awood badan oo soofoomyada ACC-yada naasleyda ah oo leh IC50 qiyam ah oo ku saabsan 55 nM. Kani hadda waa kan keliya ee la soo sheegay xannibaadaha awoodda leh ee naasleyda ACCs. Dhaqamada unugyada iyo sidoo kale moodooyinka xayawaanka, CP-640186 waxay yareyn kartaa heerarka malonyl-CoA unugyada, waxay joojin kartaa biosynthesis dufanka dufanka leh, waxayna kicin kartaa oksaydhka dufanka. Tan ugu muhiimsan, CP-640186 waxay yarayn kartaa tirada dufanka jidhka iyo miisaanka jidhka, waxayna hagaajin kartaa dareenka insulin, ansaxinta ACC-yada sida bartilmaameedyada cayilka iyo daawooyinka ka hortagga sonkorowga. |
CPD1592 | ND-630 | ND-630 waa acetyl-CoA carboxylase (ACC) inhibitor; waxay joojisaa dadka ACC1 iyo ACC2 ee leh IC50 qiyamka 2.1 iyo 6.1 nM, siday u kala horreeyaan. |