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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.
WL40 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.
WL40 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 |
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1. Song Y, et al. Leukemia. 2019 Apr 8. doi: 10.1038/s41375-019-0467-z.
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