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Cat. No.: HY-189653

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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.

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Formule: C₂₇H₃₂N₄O₂
Masse moléculaire:444.57

Stockage:

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

TEAD-IN-27 Chemical Structure

Stock

Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

TEAD1

TEAD4

Voir tous les produits spécifiques à Isoform YAP :

In Vitro

Cytokines & ChemokinesOthers

Cytokines & Chemokines

TEAD-IN-27 (compound 8) (100-500 nM; 12 h) attenuates TGF-β1-induced fibrogenic gene and protein expression in JS-1 hepatic stellate cells^[1].

Others

TEAD-IN-27 directly binds and stabilizes purified TEAD1 and TEAD4 YBD, producing ΔT_m values of 4.5 °C and 10.0 °C, respectively^[1].
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.

RT-PCR^[1]

Cell Line:

S-1 and LX-2 hepatic stellate cells
Concentration:

50 nM; 500 nM; 5000 nM
Incubation Time:

12 h
Result:

Inhibited the expression of the YAP/TAZ-TEAD target genes Ccn1, Ccn2, and Ankrd1.

Western Blot Analysis^[1]

Cell Line:

JS-1 hepatic stellate cells
Concentration:

100 nM; 500 nM
Incubation Time:

12 h
Result:

Attenuated TGF-β1-induced expression of fibrosis-related genes and proteins in JS-1 hepatic stellate cells.

In Vivo

TEAD-IN-27 (compound 8) (2.5-5 mg/kg; intraperitoneal; twice daily; one week) displays modest but measurable in vivo anti-hepatic fibrotic activity in C57BL/6JNifdc mice with CCl₄-induced hepatic fibrosis, reducing hepatic fibrogenic gene and protein markers, particularly at 5 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6JNifdc (male, 7-8 weeks old, ~22 g, SPF conditions)^[1]
Dosage:

2.5 mg/kg; 5 mg/kg
Administration:

intraperitoneal; twice daily; one week
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.

Related Protocols :

Chemical Information

Masse moléculaire 444.57
Formule C₂₇H₃₂N₄O₂
SMILES

O=C(N1CCN(C(NC2=CC=CC=C2)=O)CC1)C3=C(C=C4)C(N4CC5CCCCC5)=CC=C3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Liu X, et al. Design, synthesis, and biological evaluation of novel TEAD inhibitors for the treatment of hepatic fibrosis. European journal of medicinal chemistry. 2026 Sep 15;320:119330.

Calculators

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Molecular Weight Molecular Weight

Calculateur de dilution

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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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