KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 ke inhibitor ea molomo ea bioavailable ea apoptosis signal-regulating kinase 1 (ASK1). E khetha ASK1 ho feta ASK2 hammoho le MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, le B-RAF. E thibela keketseho e bakoang ke streptozotocin ho JNK le p38 phosphorylation ho INS-1 pancreatic β lisele ka mokhoa o itšetlehileng ka mahloriso. |
CPD100607 | K811 | K811 ke ASK1-specific inhibitor e lelefatsang ho phela ka mokhoa oa toeba oa amyotrophic lateral sclerosis. K811 e ile ea thibela ka katleho ho ata ha lisele meleng ea lisele tse nang le polelo e phahameng ea ASK1 le liseleng tsa GC tsa HER2-overexpressing. Kalafo ka K811 e fokolitse boholo ba lihlahala tsa xenograft ka ho theola matšoao a ho ata. |
CPD100606 | K812 | K812 ke ASK1-specific inhibitor e fumanoeng ho lelefatsa ho phela ka mokhoa oa toeba oa amyotrophic lateral sclerosis. |
CPD100605 | MSC-2032964A | MSC 2032964A ke ASK1 inhibitor e matla le e khethang (IC50 = 93 nM). E thibela LPS-induced ASK1 le p38 phosphorylation ho li-astrocyte tsa mouse e hlahisitsoeng le ho hatella neuroinfigueation ka mokhoa oa mouse oa EAE. MSC 2032964A e fumaneha ka molomo ebile e kenella bokong. |
CPD100604 | Selonsertib | Selonsertib, e tsejoang hape e le GS-4997, ke inhibitor ea molomo ea bioavailable ea apoptosis signal-regulating kinase 1 (ASK1), e nang le mesebetsi e ka bang khahlanong le ho ruruha, anti-antineoplastic le anti-fibrotic. GS-4997 e ipapisa le "catalytic kinase domain" ea ASK1 ka mokhoa oa tlholisano oa ATP, ka hona e thibela phosphorylation le ts'ebetso ea eona. GS-4997 e thibela tlhahiso ea li-cytokine tsa ho ruruha, ho theola-ho laola polelo ea liphatsa tsa lefutso tse amehang ho fibrosis, ho hatella apoptosis e feteletseng le ho thibela ho ata ha lisele. |