Chemical Name: 1-((1R,3S)-1-(benzo[d][1,3]dioxol-5-yl)-3-(morpholine-4-carbonyl)-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)prop-2-en-1-one. Alternate Names: (1R,3S)-2-Acryloyl-1-(benzo[d][1,3]dioxol-5-yl)-N-morpholino-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamide
Spliceosome/FOXA1 modulator
Molekulargewicht:
459.50
Reinheit:
>98% by HPLC, NMR (conforms)
Formulierung:
Pale yellow solid
CAS Nummer:
[2929223-35-6]
Formel:
C26H25N3O5
Anwendungsbeschreibung:
WX-02-23 is a spliceosome modulator. It binds to the spliceosome factor SF3B1 stabilizing a spliceosome state with enhanced binding to DDX42. WX-02-23 displayed anti-proliferative effects in Panc 05.04 and Panc 04.03 cells.1 WX-02-23 also modulates the pioneer transcription factor FOXA1 via covalent binding to Cysteine 258 in a DNA-dependent manner (EC50 = 2 µM FOXA1, 12 µM FOXA1-FKHD). It alters activity via relaxation of FOXA1s DNA-binding motif changing chromatin accessibility.2
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