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Art. -Nr.: HY-190510

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3137325-81-3
Formel: C₃₃H₂₉F₃N₄O₃
Molecular Weight:586.60

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

DF-CIV-2 Chemical Structure

CAS. Nr.: 3137325-81-3

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

TEAD2

YAP/TAZ-TEAD

Hippo

Alle YAP Isoform-spezifische Produkte anzeigen :

Alle Hippo (MST) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H226	IC50	0.078 μM	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	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.	42407407
HCT-116	IC50	0.484 μM	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.	42407407
HEK-293T	IC50	10.91 μM	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.	42407407

In Vitro

Anti-cancerOthers

Anti-cancer

DF-CIV-2 (24 h) downregulates YAP-TEAD target genes CTGF and CYR61 in NCI-H226 cells^[1].
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].

Others

DF-CIV-2 (1-fold molar excess; 24 h at 4 °C) covalently modifies recombinant TEAD2 at C380^[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.

RT-PCR^[1]

Cell Line:

NCI-H226 cells
Concentration:

62.5, 125, 250, 500 nM
Incubation Time:

24 h
Result:

Downregulated the YAP-TEAD target genes CTGF and CYR61 in NCI-H226 cells.

Cell Viability Assay^[1]

Cell Line:

NCI-H226 cells
Concentration:

0.11, 0.33, and 1 µM
Incubation Time:

24 h exposure; 72 h post-washout culture
Result:

After withdrawal, sustained suppression of NCI-H226 proliferation remained, consistent with irreversible inhibition.

Cell Migration Assay ^[1]

Cell Line:

NCI-H226 cells
Concentration:

0.25, 0.5, 1, and 2 µM
Incubation Time:

0, 24, and 48 h
Result:

Concentration-dependently suppressed NCI-H226 wound closure.

Cell Proliferation Assay^[1]

Cell Line:

NCI-H226 cells
Concentration:

0.25, 0.5, 1 µM
Incubation Time:

10 days
Result:

Concentration-dependently inhibited NCI-H226 colony formation.

Chemical Information

CAS. Nr. 3137325-81-3
Molecular Weight 586.60
Formel C₃₃H₂₉F₃N₄O₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Chen W, et al. Repurposing-inspired discovery of novel sagitta-shaped covalent TEAD inhibitors from NSAID diflunisal. European journal of medicinal chemistry. 2026 Nov 05;317:119112.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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DF-CIV-2

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