CAT # | Khoom npe | Kev piav qhia |
PIB 100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 yog qhov ncauj bioavailable inhibitor ntawm apoptosis signal-regulating kinase 1 (ASK1). Nws yog xaiv rau ASK1 tshaj ASK2 nrog rau MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, thiab B-RAF. Nws inhibits streptozotocin-induced nce nyob rau hauv JNK thiab p38 phosphorylation hauv INS-1 pancreatic β hlwb nyob rau hauv ib tug concentration-dependent yam. |
PAB 100607 | k811 ua | K811 yog ASK1 tshwj xeeb inhibitor uas ua rau muaj sia nyob ntev hauv tus qauv nas ntawm amyotrophic lateral sclerosis. K811 ua tau zoo tiv thaiv cell proliferation hauv cov kab ntawm tes nrog siab ASK1 qhia thiab hauv HER2-overexpressing GC hlwb. Kev kho mob nrog K811 txo qhov ntau thiab tsawg ntawm xenograft hlav los ntawm kev txo qis cov cim kev loj hlob. |
PIB 100606 | k812 ua | K812 yog ib qho ASK1 tshwj xeeb inhibitor tshawb pom kom muaj sia nyob ntev hauv tus qauv nas ntawm amyotrophic lateral sclerosis. |
PIB 100605 | MSC-2032964A | MSC 2032964A yog lub zog thiab xaiv ASK1 inhibitor (IC50 = 93 nM). Nws thaiv LPS-induced ASK1 thiab p38 phosphorylation hauv kab lis kev cai nas astrocytes thiab suppresses neuroinflamation hauv tus nas EAE qauv. MSC 2032964A yog qhov ncauj bioavailable thiab lub hlwb nkag mus. |
PIB 100604 | Selonsertib | Selonsertib, tseem hu ua GS-4997, yog ib qho kev hais lus bioavailable inhibitor ntawm apoptosis signal-regulating kinase 1 (ASK1), muaj peev xwm tiv thaiv kab mob, antineoplastic thiab anti-fibrotic kev ua ub no. GS-4997 lub hom phiaj thiab khi rau catalytic kinase domain ntawm ASK1 hauv kev sib tw ATP, yog li tiv thaiv nws cov phosphorylation thiab ua kom muaj zog. GS-4997 tiv thaiv kev tsim cov cytokines inflammatory, down-regulates cov kev qhia ntawm cov noob koom nrog fibrosis, suppresses ntau apoptosis thiab inhibits cellular proliferation. |