| Ologbo # | Orukọ ọja | Apejuwe |
| CPD100608 | ASK1-Idanujẹ-10 | ASK1 Inhibitor 10 jẹ onidalẹkun ti ẹnu bioavailable ti ifihan apoptosis ti n ṣakoso kinase 1 (ASK1). O jẹ yiyan fun ASK1 lori ASK2 bakanna bi MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ati B-RAF. O ṣe idiwọ awọn ilọsiwaju ti streptozotocin-induced ni JNK ati p38 phosphorylation ninu awọn sẹẹli β pancreatic INS-1 ni ọna ti o gbẹkẹle ifọkansi. |
| CPD100607 | K811 | K811 jẹ onidalẹkun pato-ASK1 ti o fa iwalaaye pẹ ni awoṣe Asin ti sclerosis ita gbangba amyotrophic. K811 ṣe idiwọ ilọsiwaju sẹẹli daradara ni awọn laini sẹẹli pẹlu ikosile ASK1 giga ati ni awọn sẹẹli GC ti HER2-overexpressing. Itọju pẹlu K811 dinku awọn iwọn ti awọn èèmọ xenograft nipasẹ isọdọtun awọn ami isunmọ. |
| CPD100606 | K812 | K812 jẹ onidalẹkun pato-ASK1 ti a ṣe awari lati pẹ iwalaaye ni awoṣe Asin ti sclerosis ita gbangba amyotrophic. |
| CPD100605 | MSC-2032964A | MSC 2032964A jẹ apaniyan ASK1 ti o lagbara ati yiyan (IC50 = 93 nM). O ṣe idiwọ ASK1 ti o fa LPS ati p38 phosphorylation ninu awọn astrocytes asin ti gbin ati ki o dinku neuroinflammation ni awoṣe EAE Asin kan. MSC 2032964A jẹ bioavailable ẹnu ati penetrant ọpọlọ. |
| CPD100604 | Selonsertib | Selonsertib, tun mo bi GS-4997, jẹ ẹya orally bioavailable onidalẹkun ti apoptosis ifihan agbara-regulating kinase 1 (ASK1), pẹlu o pọju egboogi-iredodo, antineoplastic ati egboogi-fibrotic akitiyan. Awọn ibi-afẹde GS-4997 ati sopọ si agbegbe catalytic kinase ti ASK1 ni ọna ifigagbaga-ATP, nitorinaa idilọwọ awọn fosforeli ati imuṣiṣẹ rẹ. GS-4997 ṣe idiwọ iṣelọpọ ti awọn cytokines iredodo, isalẹ-ilana ikosile ti awọn Jiini ti o ni ipa ninu fibrosis, dinku apoptosis ti o pọ ju ati ṣe idiwọ ilọsiwaju cellular. |
