DF-CIV-2
DF-CIV-2 is a TEAD2 inhibitor. DF-CIV-2 covalently modifies the TEAD2 palmitoylation pocket, inhibiting TEAD2 palmitoylation and YAP-TEAD binding. DF-CIV-2 inhibits YAP/TAZ-TEAD transcriptional output and downregulates Hippo target genes. DF-CIV-2 can be used for research on malignant mesothelioma.
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- No. CAS: 3137325-81-3
- Fòrmula: C33H29F3N4O3
- Peso molecular:586.60
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
TEAD2 |
YAP/TAZ-TEAD |
Hippo |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H226 | IC50 |
0.078 μM
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Antiproliferative activity against human NCI-H226 cells assessed as viability reduction incubated 96 hrs by CCK8 assay.
Antiproliferative activity against human NCI-H226 cells assessed as viability reduction incubated 96 hrs by CCK8 assay.
|
42407407 |
| MDA-MB-231 | IC50 |
3.243 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
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42407407 |
| HCT-116 | IC50 |
0.484 μM
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Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
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42407407 |
| HEK-293T | IC50 |
10.91 μM
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Antiproliferative activity against human HEK293T cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
Antiproliferative activity against human HEK293T cells assessed as viability reduction incubated 72 hrs by CCK8 assay.
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42407407 |
In Vitro
DF-CIV-2 (1 µM; 24 h) broadly suppresses YAP/TAZ-TEAD transcriptional programs in NCI-H226 cells[1].
DF-CIV-2 (Gradient concentrations; 72-96 h) selectively inhibits proliferation of YAP-dependent NCI-H226 cells with an IC50 of 0.078 µM[1].
DF-CIV-2 (0.11-1 µM; 24-72 h) produces sustained antiproliferative effects in NCI-H226 cells after washout[1].
DF-CIV-2 (0.25-2 µM; 0-48 h) inhibits NCI-H226 cell migration in a concentration-dependent manner[1].
DF-CIV-2 (Indicated doses; 10 days) suppresses colony-forming ability of NCI-H226 cells[1].
DF-CIV-2 (0.25-2 µM; 18 days) inhibits NCI-H226 3D tumor spheroid growth in a concentration-dependent manner[1].
DF-CIV-2 (Six doses; day 4) synergizes with MEK, PI3Kα, and mTORC1 inhibitors in NCI-H226 mesothelioma cells[1].
DF-CIV-2 (6-4500 nM; 2 h) inhibits TEAD2 palmitoylation in vitro across 6-4500 nM[1].
DF-CIV-2 (0.16-10 µM; 2 h) reduces YAP-TEAD2 association in a concentration-dependent pull-down assay[1].
DF-CIV-2 (Gradient concentrations; 24 h) potently inhibits TEAD transcriptional activity in HEK-293T reporter cells with an IC50 of 21.8 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H226 cells
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Concentration:62.5, 125, 250, 500 nM
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Incubation Time:24 h
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Result:Downregulated the YAP-TEAD target genes CTGF and CYR61 in NCI-H226 cells.
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Cell Line:NCI-H226 cells
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Concentration:0.11, 0.33, and 1 µM
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Incubation Time:24 h exposure; 72 h post-washout culture
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Result:After withdrawal, sustained suppression of NCI-H226 proliferation remained, consistent with irreversible inhibition.
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Cell Line:NCI-H226 cells
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Concentration:0.25, 0.5, 1, and 2 µM
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Incubation Time:0, 24, and 48 h
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Result:Concentration-dependently suppressed NCI-H226 wound closure.
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Cell Line:NCI-H226 cells
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Concentration:0.25, 0.5, 1 µM
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Incubation Time:10 days
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Result:Concentration-dependently inhibited NCI-H226 colony formation.
Chemical Information
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No. CAS 3137325-81-3
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Peso molecular 586.60
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Fòrmula C33H29F3N4O3
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SMILES
O=C(NC1=CC(C(C=CC=C2)=C2OC3=CC=C(C=C3)C(F)(F)F)=CC(N4CCN(CC4)C(NC5=CC=CC=C5)=O)=C1)C=C
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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)
DF-CIV-2 Related Classifications
HY-190510 Related Classifications
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