IKATI # | Igama Lomkhiqizo | Incazelo |
I-CPD100608 | ASK1-Inhibitor-10 | I-ASK1 Inhibitor 10 iyi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1). Iyakhetha ku-ASK1 phezu kwe-ASK2 kanye ne-MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ne-B-RAF. Ivimbela ukwanda kwe-streptozotocin-induced ku-JNK kanye ne-p38 phosphorylation kumaseli we-INS-1 we-pancreatic β ngendlela encike ekugxilweni. |
I-CPD100607 | K811 | I-K811 iyisivimbeli esiqondene ne-ASK1 esandisa isikhathi sokusinda kumodeli yegundane ye-amyotrophic lateral sclerosis. I-K811 ivimbele ngempumelelo ukwanda kwamaseli kolayini beseli abanesisho esiphezulu esingu-ASK1 kanye namaseli e-GC e-HER2-overexpressing overexpressing. Ukwelashwa nge-K811 kuncishiswe osayizi bamathumba e-xenograft ngokwehlisa izimpawu zokusabalala. |
I-CPD100606 | K812 | I-K812 iyisivimbeli esiqondene ne-ASK1 esitholwe ukwandisa isikhathi sokusinda kumodeli yegundane ye-amyotrophic lateral sclerosis. |
I-CPD100605 | I-MSC-2032964A | I-MSC 2032964A iyi-ASK1 inhibitor enamandla futhi ekhethayo (IC50 = 93 nM). Ivimba i-ASK1 eyenziwe nge-LPS kanye ne-p38 phosphorylation kuma-astrocyte egundane elikhulisiwe futhi icindezela ukuvuvukala kwe-neuroinflammation kumodeli ye-EAE yegundane. I-MSC 2032964A iyatholakala nge-bioavailable ngomlomo futhi ingena ebuchosheni. |
I-CPD100604 | I-Selonsertib | I-Selonsertib, eyaziwa nangokuthi i-GS-4997, iyi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1), enekhono lokulwa nokuvuvukala, i-antineoplastic kanye ne-anti-fibrotic. I-GS-4997 iqondisa futhi ibophezela kusizinda se-catalytic kinase se-ASK1 ngendlela yokuncintisana ye-ATP, ngaleyo ndlela ivimbele ukwenziwa kwayo kwe-phosphorylation nokwenziwa kusebenze. I-GS-4997 ivimbela ukukhiqizwa kwama-cytokines avuthayo, ilawula phansi ukubonakaliswa kwezakhi zofuzo ezihilelekile ku-fibrosis, icindezela i-apoptosis ngokweqile futhi ivimbele ukwanda kwamaselula. |