2933893-27-5
Chemical Structure
GNE-8025
- CAS No.: 2933893-27-5
- Formula:C19H17F3N4O4
- Molecular Weight:422.36
InChIKey: AAYVOUUBHRKCMZ-OAHLLOKOSA-N
SMILES: C=CC(NCC1=NN(C2=C1C([C@@H](CO)O)=CC=N2)C3=CC=C(C=C3)OC(F)(F)F)=O
Biological Activity: GNE-8025 is an orally active pan-TEAD transcription factor inhibitor, with IC50 values of 45, 38, 1035 and 24 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8025 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8025 suppresses YAP-driven tumor cell growth. GNE-8025 enhances the activity of MAPK and KRASG12C inhibitors. GNE-8025 can be used for the research of pleural mesothelioma and KRASG12C-mutant cancers[1].
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GNE-8025 | GNE-8025 is an orally active pan-TEAD transcription factor inhibitor, with IC50 values of 45, 38, 1035 and 24 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8025 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8025 suppresses YAP-driven tumor cell growth. GNE-8025 enhances the activity of MAPK and KRASG12C inhibitors. GNE-8025 can be used for the research of pleural mesothelioma and KRASG12C-mutant cancers. | |||||||||||||||||||||
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Keywords
