MPAKA # | Dzina lazogulitsa | Kufotokozera |
CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 ndi orally bioavailable inhibitor ya apoptosis signal-regulating kinase 1 (ASK1). Imasankha ASK1 pa ASK2 komanso MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ndi B-RAF. Imalepheretsa kuwonjezeka kwa streptozotocin-induced mu JNK ndi p38 phosphorylation mu INS-1 pancreatic β maselo m'njira yodalira ndende. |
Chithunzi cha CPD100607 | K811 | K811 ndi ASK1-specific inhibitor yomwe imatalikitsa kupulumuka mu mtundu wa mbewa wa amyotrophic lateral sclerosis. K811 imalepheretsa bwino kuchulukana kwa maselo m'maselo okhala ndi mawu apamwamba a ASK1 komanso ma cell a HER2-overexpressing GC. Kuchiza ndi K811 kumachepetsa kukula kwa zotupa za xenograft pochepetsa zolembera za kuchuluka. |
Chithunzi cha CPD100606 | K812 | K812 ndi ASK1-specific inhibitor yomwe yapezedwa kuti italikitse kupulumuka mu mtundu wa mbewa wa amyotrophic lateral sclerosis. |
Chithunzi cha CPD100605 | MSC-2032964A | MSC 2032964A ndi yamphamvu komanso yosankha ASK1 inhibitor (IC50 = 93 nM). Imaletsa LPS-induced ASK1 ndi p38 phosphorylation mu astrocyte otukuka a mbewa ndikupondereza neuroinflammation mumtundu wa EAE wa mbewa. MSC 2032964A ndi bioavailable pakamwa komanso kulowa muubongo. |
Chithunzi cha CPD100604 | Selonsertib | Selonsertib, yomwe imadziwikanso kuti GS-4997, ndi inhibitor yapakamwa ya bioavailable ya apoptosis sign-regulating kinase 1 (ASK1), yokhala ndi anti-yotupa, anti-antineoplastic komanso anti-fibrotic. GS-4997 imayang'ana ndikumanga ku catalytic kinase domain ya ASK1 mumpikisano wa ATP, potero imalepheretsa phosphorylation ndi kutsegula kwake. GS-4997 imalepheretsa kupanga ma cytokines otupa, kutsika-kuwongolera mawonekedwe a majini omwe amakhudzidwa ndi fibrosis, kupondereza apoptosis kwambiri ndikuletsa kuchuluka kwa ma cell. |