OPN-9643
OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma.
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- No. CAS: 2866423-06-3
- Fòrmula: C19H16F3NO2
- Peso molecular:347.33
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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TEAD 15 nM (IC50) |
OPN-9643 (2 µM; 24-48 h) reduces the expression of TEAD targets (CTGF and CYR61) in SOX10 KO cells. OPN-9643 reduces luciferase activity. OPN-9643 reduces other known TEAD targets, such as DKK1, MYC, and TGF-β2 in SOX10 KO melanoma cells[1].\nOPN-9643 (NCI-H226 cells; 5 days) inhibits TEAD activity and cell growth (IC50 of 123 nM) in NCI-H226 cells[1].
When administered in combination with BRAFi (BRAF inhibitor) + MEKi (MEK inhibitor), and OPN-9643 (2 μM; 48-72 h) markedly decreases cell growth in A375 SOX10 KO cells compared to BRAFi + MEKi alone[1].
OPN-9643 (2 μM; 48 h) increases the cleaved-PARP and cleaved-GSDME in the combination treated SOX10 KO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 parental, A375 crSOX10 #2.18, and A375 crSOX10 #4.21 cells
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Concentration:2 μM
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Incubation Time:24 h, 48 h
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Result:Western blotting analysis detected a reduction in CTGF and CYR61 protein expression in SOX10 KO cells.
Down-regulated the cell cycle progression regulators (FOXM1 and PLK1), growth factor receptors (phospho-cMET Y1234/5, AXL), a serine protease inhibitor (PAI1), and RAD51.
Chemical Information
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No. CAS 2866423-06-3
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Peso molecular 347.33
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Fòrmula C19H16F3NO2
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SMILES
C=CC(N1CC2=C(C=CC(OC3=CC=C(C(F)(F)F)C=C3)=C2)CC1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OPN-9643 Related Classifications
HY-179559 Related Classifications
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