2933893-78-6
Chemical Structure
GNE-2181
- CAS. Nr.: 2933893-78-6
- Formula:C20H16F4N4O3
- Molecular Weight:436.36
InChIKey: PWQJFURIOYPGCQ-UHFFFAOYSA-N
SMILES: C=C(C(N1CC(C1)C2=NN(C3=C2C(CO)=CC=N3)C4=CC=C(C=C4)OC(F)(F)F)=O)F
Biological Activity: 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[1].
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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. | |||||||||||||||||||||
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Keywords
