WDR5 PROTAC MS40 | WDR5 PROTAC | Probechem Biochemicals

Chemical Structure : WDR5 PROTAC MS40

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WDR5 PROTAC MS40 (MS40)

货号: PC-49061Not For Human Use, Lab Use Only.

WDR5 PROTAC MS40 is a cereblon (CRBN)-recruiting proteolysis targeting chimera (PROTAC) of WDR5, selectively degrades WDR5 and the Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3.

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生物&药学活性

WDR5 PROTAC MS40 is a cereblon (CRBN)-recruiting proteolysis targeting chimera (PROTAC) of WDR5, selectively degrades WDR5 and the Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3.
MS40-induced WDR5 degradation caused disassociation of the MLL/KMT2A complex off chromatin, resulting in decreased H3K4me2.
MS40 repressed transcriptomic profiling revealed that targets of both WDR5 and the well-established neo-substrates of immunomodulatory drugs (IMiDs):CRBN.
MS40 suppressed the growth of primary leukemia patient cells in vitro and patient-derived xenografts in vivo.
MS40 is superior in suppressing oncogenesis to the WDR5 PPI inhibitor and to VHL-based WDR5 PROTAC (MS169, which degrades WDR5 but not Ikaros).

物理化学性质&存储条件

分子量	995.118
分子式	C52H61F3N10O7
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-[3′-[[4-[2-[[8-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-1-oxooctyl]amino]ethyl]-1-piperazinyl]methyl]-4-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-3-yl]-1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinecarboxamide

参考文献

1. Li D, et al. Oncogene. 2022 Jun;41(24):3328-3340.

WDR5 PROTAC MS40 (MS40)

生物&药学活性

物理化学性质&存储条件

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WDR5 PROTAC MS40 (MS40)

生物&药学活性

物理化学性质&存储条件

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