Rpn13 degrader WL40 | Rpn13 PROTAC | Probechem Biochemicals

Chemical Structure : Rpn13 degrader WL40

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Rpn13 degrader WL40 (WL40)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	1019.751
分子式	C50H47Cl4N5O10
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

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

Rpn13 degrader WL40 (WL40)

生物&药学活性

物理化学性质&存储条件

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Rpn13 degrader WL40 (WL40)

生物&药学活性

物理化学性质&存储条件

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