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Product Information:

GNE-2181

GNE-2181 is an orally active, blood-brain barrier-penetrant pan-TEAD transcription factor inhibitor, with IC50 values of 13, 26, 61 and 17 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8021 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8021 suppresses YAP-driven tumor cell growth. GNE-2181 inhibits the growth of intracranial tumor models in vivo. GNE-2181 can be used for research on brain metastasis of lung cancer .

Cat. No.: EX-A17412    Purity: >98%
Chemical
Chemical structure of GNE-2181


For research only, Do not use for Human!

SizeUnit Price (US$)StockQuantityOrder
5mg495Inquire
10mg795Inquire


CAS No.2933893-78-6
Purity>98%
FormulaC20H16F4N4O3
Mol Weight436.3597
 
 
Reference:  

[1].Hagenbeek TJ, et al. Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in a Hippo-dependent cancer model. Nature communications. 2026 Jun 27.

CoACoA of GNE-2181
Smiles:C=C(C(N1CC(C1)C2=NN(C3=C2C(CO)=CC=N3)C4=CC=C(C=C4)OC(F)(F)F)=O)F

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