nwamba # | Aha ngwaahịa | Nkọwa |
CPD100573 | PF-05175157 | PF-05175157 bụ onye na-egbochi ike na nhọrọ nke ma acetyl-CoA carboxylase isoform ACC1 nke dị na imeju na anụ ahụ adipose na isoform ACC2 na-achịkwa na skeletal na obi obi, yana ụkpụrụ IC50 nke 27 nM na 33 nM, n'otu n'otu. Ndị inhibitors ACC na-egbochi de novo lipogenesis ma na-abawanye β-oxidation nke ọdụdụ ọdụdụ ọdụdụ asịd nwere ike ịgwọ ụdị ọrịa shuga 2, steatosis imeju, na ọrịa kansa. |
CPD100572 | ND-646 | ND-646 bụ allosteric inhibitor nke ACC enzymes ACC1 na ACC2 na-egbochi ACC subunit dimerization-iji kwụsị njikọ fatty acid in vitro na in vivo. Ọgwụgwọ ND-646 na-adịghị ala ala nke xenograft na ụdị òké ejiri mkpụrụ ndụ ihe nketa nke NSCLC gbochiri uto etuto. Mgbe a na-elekọta ya dị ka otu onye nnọchi anya ma ọ bụ yana yana ọgwụ carboplatin na-ahụ maka nlekọta, ND-646 na-ebelata oke etuto ngụgụ na Kras;Trp53-/- (nke a makwaara dị ka KRAS p53) na Kras; Stk11-/- ( makwaara dị ka KRAS Lkb1) ụdị òké nke NSCLC. ND-646 emeela ka ọ dị mma mgbe ejikọtara ya na carboplatin, otu akụkụ nke usoro ọgwụgwọ chemotherapeutic eji agwọ NSCLC mmadụ. |
CPD100571 | CP-640186 | CP-640186 bụ ihe mgbochi siri ike nke ACC mammalian ma nwee ike ibelata ibu ahụ yana melite mmetụta insulin na anụmanụ ule. CP-640186 ka egosiri n'oge na-adịbeghị anya dị ka onye na-egbochi isoforms nke ACC mammalian nwere ụkpụrụ IC50 nke ihe dịka 55 nM. Nke a bụ naanị ihe mgbochi nwere ike na-egbochi ACC mammalian. Na omenala cell yana ụdị anụmanụ, CP-640186 nwere ike ibelata ọkwa malonyl-CoA anụ ahụ, na-egbochi biosynthesis fatty acid, ma kpalie acid oxidation fatty acid. Nke kachasị mkpa, CP-640186 nwere ike ibelata oke abụba anụ ahụ na ịdị arọ ahụ, ma melite mmetụta insulin, na-akwado ACC dị ka ebumnuche maka mgbochi oke ibu na ọgwụ antidiabetes. |
CPD1592 | ND-630 | ND-630 bụ ihe mgbochi acetyl-CoA carboxylase (ACC); na-egbochi mmadụ ACC1 na ACC2 na ụkpụrụ IC50 nke 2.1 na 6.1 nM, n'otu n'otu. |