CAT # | Igama lemveliso | Inkcazo |
CPD100608 | ASK1-Inhibitor-10 | I-ASK1 Inhibitor 10 yi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1). Ikhetha i-ASK1 phezu kwe-ASK2 kunye ne-MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, kunye ne-B-RAF. Ivimbela ukunyuka okubangelwa yi-streptozotocin kwi-JNK kunye ne-p38 phosphorylation kwi-INS-1 i-pancreatic β cells ngendlela exhomekeke kuyo. |
CPD100607 | K811 | I-K811 yi-ASK1-specific inhibitor eyenza ixesha elide ukusinda kwimodeli ye-mouse ye-amyotrophic lateral sclerosis. I-K811 ikhusele ngokufanelekileyo ukwanda kweeseli kwimizila yeeseli kunye nenkcazo ephezulu ye-ASK1 kunye nakwiiseli ze-GC ze-HER2-overexpressing. Unyango nge-K811 lucuthe ubungakanani bamathumba e-xenograft ngokunciphisa iimpawu zokwanda. |
CPD100606 | K812 | I-K812 yi-ASK1-specific inhibitor efunyenwe ukwandisa ukusinda kwimodeli ye-mouse ye-amyotrophic lateral sclerosis. |
CPD100605 | I-MSC-2032964A | I-MSC 2032964A inamandla kwaye i-ASK1 inhibitor ekhethiweyo (IC50 = 93 nM). Ivimba i-ASK1 eyenziwe yi-LPS kunye ne-p38 phosphorylation kwi-astrocyte yemouse ekhuliswe kwaye icinezela i-neuroinflammation kwimodeli ye-EAE ye mouse. I-MSC 2032964A ifumaneka ngomlomo kwaye ingena ebuchotsheni. |
CPD100604 | Selonsertib | I-Selonsertib, eyaziwa ngokuba yi-GS-4997, yi-inhibitor ye-bioavailable yomlomo ye-apoptosis ye-signal-regulating kinase 1 (ASK1), ene-anti-inflammatory, i-antineoplastic kunye ne-anti-fibrotic imisebenzi. Iithagethi ze-GS-4997 kwaye zibophelela kwi-catalytic kinase domain ye-ASK1 ngendlela ye-ATP-ekhuphisanayo, ngaloo ndlela ikhusela i-phosphorylation kunye nokusebenza kwayo. I-GS-4997 ikhusela ukuveliswa kwee-cytokines ezivuthayo, i-down-ilawula ukubonakaliswa kwezakhi zofuzo ezibandakanyekayo kwi-fibrosis, icinezela i-apoptosis eninzi kwaye inqanda ukwanda kwamaselula. |