Rpn13 degrader WL40

Research use only, not for human use.

Rpn13 degrader WL40 (WL40) is a novel covalent ubiquitin receptor Rpn13 degrader by linking the Rpn13 covalent inhibitor RA190 with the cereblon (CRBN) binding ligand thalidomide.

Rpn13 degrader WL40 (WL40) is a novel covalent ubiquitin receptor Rpn13 degrader by linking the Rpn13 covalent inhibitor RA190 with the cereblon (CRBN) binding ligand thalidomide; binds to both Rpn13 and CRBN and triggers degradation of cellular Rpn13; WL40 decreases viability in MM cell lines and patient MM cells (IC50=400-750 nM), even those resistant to bortezomib, WL40 interrupts Rpn13 function and activates caspase apoptotic cascade, ER stress response and p53/p21 signaling; inhibits xenografted human MM cell growth and prolongs survival in animal model studies.

WL40

PROTACs

PROTAC

PROTAC

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1019.75

C50H47Cl4N5O10

>98% (HPLC)

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N-((S)-1-(3,5-bis((Z)-3,4-dichlorobenzylidene)-4-oxopiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)-3-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)propanamide

(-20℃)

With Ice Pack

≥ 2 years