Chemical Structure : Rpn13 degrader WL40
Catalog No.: PC-36168Not For Human Use, Lab Use Only.
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.
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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.
M.Wt | 1019.751 | |
Formula | C50H47Cl4N5O10 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Song Y, et al. Leukemia. 2019 Apr 8. doi: 10.1038/s41375-019-0467-z.
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