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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-GNE-2181
GNE-2181

Chemical Structure : GNE-2181

CAS No.: 2933893-78-6

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GNE-2181 (GNE2181)

货号: PC-27127Not For Human Use, Lab Use Only.

GNE-2181 is a potent, selective, covalent, orally bioavailable and brain-penetrant pan-TEAD inhibitor, disrupts YAP-TEAD interaction with biochemical IC50s of 2/4/8/6 nM for TEAD1/2/3/4 in TR-FRET assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GNE-2181 is a potent, selective, covalent, orally bioavailable and brain-penetrant pan-TEAD inhibitor, disrupts YAP-TEAD interaction with biochemical IC50s of 2/4/8/6 nM for TEAD1/2/3/4 in TR-FRET assays.
GNE-2181 bind potently and covalently to the lipid pocket of TEAD proteins, form a covalent linkage with the lipid pocket cysteine (C380) of TEAD2 through the acrylamide warhead.
GNE-2181 exhibits strong activity against all four isoforms of TEAD.
GNE-2181 potently inhibits cell proliferation of Hippo-driven cell lines NCI-H226 and MSTO-211H with EC50 of 3 nM and 7 nM, but not Hippo-independent VMRC-LCD cells with >2500-fold higher EC50 values.
GNE-2181 shows superior efficacy in both NCI-H226 and MSTO-211H cells versus GNE-6915 and GNE-7883, downregulates YAP/TAZ–TEAD-dependent gene programs to exert anti-proliferative effects.
GNE-2181 enhances the efficacy of targeted cancer therapies, particularly when combined with inhibitors of RTKs and the RAS/MAPK pathway.
GNE-2181 (10 or 50 mg/kg) effectively inhibited brain tumor growth in brain metastasis with advanced stage lung cancer NCI-H226, with a concomitant reduction of the YAP/TAZ target score and proliferation marker (Ki67).

物理化学性质&存储条件

分子量 436.37
分子式 C20H16F4N4O3
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

2-fluoro-1-(3-(4-(hydroxymethyl)-1-(4-(trifluoromethoxy)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)azetidin-1-yl)prop-2-en-1-one

参考文献

1. Hagenbeek TJ, et al. Nat Commun. 2026 Jun 27. doi: 10.1038/s41467-026-74722-5.

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