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Biochem/physiol Actions
MYF-03-176 is an orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP-TEAD association by targeting TEAD palmitate pocket for covalent binding. MYF-03-176 suppresses NCI-H226 cellular TEAD transcriptional activity (IC50 = 11 nM by TEAD reporter assay), blocking TEAD-mediated target genes expression (CTGF, CYR61, ANKRD1) and suppression (BMF). MYF-03-176 effectively inhibits Hippo signaling-driven human lung mesothelioma NCI-H226 proliferaton in cultures (IC50 = 9 nM in 5 days) and in a xenograft model in mice in vivo (35 or 75 mg/kg b.i.d. p.o. for 4 wks).
Orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP-TEAD association and inhibits Hippo signaling-driven cancer proliferation in vitro and in vivo.
Disclaimer
Hygroscopic
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
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¥ 805.47
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¥ 711.69
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¥ 1669.50
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