TEAD-IN-27
TEAD-IN-27 is a TEAD1-4 inhibitor that inhibits TEAD-dependent transcriptional activity. TEAD-IN-27 directly binds to and stabilizes TEAD1 and TEAD4, and binds purified TEAD protein in thermal shift assays. TEAD-IN-27 inhibits hepatic stellate cell activation and fibrotic gene expression, and alleviates chemically induced liver fibrosis and extracellular matrix deposition. TEAD-IN-27 can be used for research on liver fibrosis.
For research use only. We do not sell to patients.
- Formula: C27H32N4O2
- Molecular Weight:444.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All YAP Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
TEAD1 |
TEAD4 |
In Vitro
TEAD-IN-27 (1-10 μM; 16-18 h) inhibits YAP/TAZ-TEAD transcriptional activity in HEK293T 8×GTIIC-luciferase reporter cells with an IC50 of 180.7 nM[1].
TEAD-IN-27 (Eight serial concentrations; 16-18 h) exhibits pan-TEAD inhibitory activity in COS-7 GAL4-TEAD1-4 reporter cells with IC50 values ranging from 159.1 to 453.1 nM[1].
TEAD-IN-27 (12 h) suppresses YAP/TAZ-TEAD target gene expression in JS-1 and LX-2 hepatic stellate cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:S-1 and LX-2 hepatic stellate cells
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Concentration:50 nM; 500 nM; 5000 nM
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Incubation Time:12 h
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Result:Inhibited the expression of the YAP/TAZ-TEAD target genes Ccn1, Ccn2, and Ankrd1.
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Cell Line:JS-1 hepatic stellate cells
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Concentration:100 nM; 500 nM
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Incubation Time:12 h
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Result:Attenuated TGF-β1-induced expression of fibrosis-related genes and proteins in JS-1 hepatic stellate cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6JNifdc (male, 7-8 weeks old, ~22 g, SPF conditions)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:intraperitoneal; twice daily; one week
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Result:Serum ALT and AST levels showed a downward trend in mice given TEAD-IN-27 (compound 8) compared with the CCl4 model group.
Reduced expression of Vim, Col1a1, Fn1, Acta2, and Col3a1.
Reduced FN1 and α-SMA protein levels.
Resulted in a modest reduction in collagen staining by Sirius Red.
Did not markedly restore overall tissue damage by H&E staining.
- RT-PCR
- Fibrosis/Collagen Morphometry
- Dual Luciferin reporter gene assay
- RNA extraction experimental
- Collagen: Sirius Red Staining
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- ECM-Embedded Organoid (Matrigel/Dome) Culture
- Matrigel/ECM Transwell Invasion Assay
- Real Time qPCR (Q-PCR)
- Liver Histomorphometry
- Matrigel Transwell/Boyden Chamber Invasion Assay
Chemical Information
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Molecular Weight 444.57
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Formula C27H32N4O2
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SMILES
O=C(N1CCN(C(NC2=CC=CC=C2)=O)CC1)C3=C(C=C4)C(N4CC5CCCCC5)=CC=C3
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)