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首页-抗体药物偶连体和PROTACs-PROTAC-MS7131
MS7131

Chemical Structure : MS7131

CAS No.:

MS7131

货号: PC-24383Not For Human Use, Lab Use Only.

MS7131 is a first-in-class USP1-recruiting UTX (KDM6A, Ubiquitously transcribed tetratricopeptide repeat X chromosome) deubiquitinase-targeting chimera (DUBTAC), selectively stabilizes the tumor suppressor UTX, but not the oncoprotein JMJD3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MS7131 is a first-in-class USP1-recruiting UTX (KDM6A, Ubiquitously transcribed tetratricopeptide repeat X chromosome) deubiquitinase-targeting chimera (DUBTAC), selectively stabilizes the tumor suppressor UTX, but not the oncoprotein JMJD3.
MS7131 stabilizes UTX in a concentration-, time-, UTX- and USP1-dependent manner without altering the UTX mRNA expression.
MS7131 selectively stabilized UTX without affecting the JMJD3 protein level, yet still maintaining sufficient potency to inhibit the enzymatic activity of the oncoprotein JMJD3.
MS7131 effectively reduced H3K27 trimethylation (H3K27me3) and inhibited cancer cell proliferation in cell viability (HCT116 cell IC50=5.6 uM) and clonogenicity assays.

物理化学性质&存储条件

分子量 978.21
分子式 C55H67N11O6
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

ethyl 3-((2-(4-(14-methyl-1-(2-(5-methyl-4-((pyridin-3-ylmethyl)amino)pyrimidin-2-yl)phenyl)-3,13-dioxo-7,10-dioxa-4,14-diazaheptadecan-17-yl)pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoate

参考文献

1. Qian C, et al. J Am Chem Soc. 2025 Apr 19. doi: 10.1021/jacs.5c01662.

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