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.
For research use only. We do not sell to patients.
- CAS No.: 2866423-06-3
- Formula: C19H16F3NO2
- Molecular Weight:347.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
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Biological Activity
Description
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TEAD 15 nM (IC50) |
In Vitro
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. Further protocols information, click here.
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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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CAS No. 2866423-06-3
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Molecular Weight 347.33
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OPN-9643 Related Classifications
HY-179559 Related Classifications
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