MS132 | WDR5 PROTAC | Probechem Biochemicals

Chemical Structure : MS132

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MS132 (WDR5 PROTAC MS132)

货号: PC-21507Not For Human Use, Lab Use Only.

MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.

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生物&药学活性

MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.
MS132 shows high binding affinities to both VCB E3 ligase (KD= 534 ± 48 nM) and WDR5 (KD= 122 ± 56 nM) in ITC assays.
MS132 induces WDR5 degradation in a concentration-, time-, and UPS-dependent manner in PDAC cells.
MS132 exhibits antiproliferative activity in multiple PDAC cell lines including MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05, and PANC-1, with GI50 of 4-32 uM.
MS132 has the potential to be used in in vivo animal studies.

物理化学性质&存储条件

分子量	1016.13
分子式	C51H57F4N9O7S
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-(2'-Fluoro-5'-((2-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethyl)carbamoyl)-4-((3S,5R)-3,4,5-trimethylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide

参考文献

1. Xufen Yu, et al. J Med Chem. 2023.

MS132 (WDR5 PROTAC MS132)

生物&药学活性

物理化学性质&存储条件

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MS132 (WDR5 PROTAC MS132)

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物理化学性质&存储条件

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