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Art. -Nr.: HY-183753

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LC-TD-05

LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC₅₀ values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC₅₀ of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₇H₂₃F₃N₄O₂
Molecular Weight:492.49

Speicherung:

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

LC-TD-05 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

TEAD4

68.3 nM (IC₅₀)

TEAD1

116.6 nM (IC₅₀)

TEAD2

168.7 nM (IC₅₀)

TEAD3

1261.0 nM (IC₅₀)

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In Vitro

LC-TD-05 (72 h) selectively inhibits the proliferation of HCC LM3, SK-HEP-1, HepG2 and Huh7 cells, with IC₅₀ values of 248 nM, 964 nM, 7.108 μM and 4.603 μM, respectively. It exhibits extremely low cytotoxicity toward non-tumorigenic HEK293T and THLE-2 cells^[1].
LC-TD-05 (3 μM; 10-14 d) potently inhibits colony formation of HCC LM3 cells^[1].
LC-TD-05 (0.3-10 μM; 3 h) downregulates the mRNA expression of TEAD target genes CTGF and CYR61 in HCC LM3 cells in a dose-dependent manner^[1].
LC-TD-05 (3-10 μM; 72 h) dose-dependently induces apoptosis in hepatocellular carcinoma LM3 cells^[1].
LC-TD-05 inhibits TEAD-associated transcriptional programs in HCC LM3 cells, including downregulation of cell cycle progression genes and canonical TEAD target genes^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HCC LM3 cells
Concentration:

3 μM
Incubation Time:

10-14 days
Result:

Significantly reduced the number of colonies formed by HCC LM3 cells compared to DMSO control.

Real Time qPCR^[1]

Cell Line:

HCC LM3 cells
Concentration:

0.3, 1, 3 and 10 μM
Incubation Time:

3 hours
Result:

Significantly downregulated the mRNA expression of CTGF and CYR61 in a dose-dependent manner, with maximal suppression at 10 μM.

Apoptosis Analysis^[1]

Cell Line:

HCC LM3 cells
Concentration:

3 and 10 μM
Incubation Time:

72 hours
Result:

Induced a dose-dependent increase in the proportion of apoptotic HCC LM3 cells, with significant elevation at 3 μM and 10 μM compared to DMSO control.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	CL	MRT_0-∞	T_1/2	T_max	F
Rat^[1]	1 mg/kg	i.v.	667 ng/mL	2536 ng·h/mL	467 mL/h/kg	6.99 h	5.60 h	/	/
Rat^[1]	10 mg/kg	p.o.	1313 ng/mL	13616 ng·h/mL	/	7.46 h	5.54 h	2.00 h	53.7 %

In Vivo

LC-TD-05 (50 mg/kg; i.p.; once daily; for 17 consecutive days) exhibits significant in vivo anti-tumor activity in the HCC LM3 xenograft model^[1].

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

Animal Model:

BALB/c nude (male, 4-6 weeks old)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; once daily; 17 days
Result:

Achieved a tumor growth inhibition (TGI) of 75%.
Markedly reduced tumor weights compared to vehicle controls.
Showed no significant change in body weight relative to the vehicle group.
Reduced protein and transcript levels of the TEAD target genes CTGF and CYR61 in treated tumor tissues.

Chemical Information

Molecular Weight 492.49
Formel C₂₇H₂₃F₃N₄O₂
SMILES

O=C(N1CCN(C(C2=CC=CC3=C2C=CN3C4=CC=C(C(F)(F)F)C=C4)=O)CC1)NC5=CC=CC=C5
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]. Xu D, et al. Discovery and optimization of novel TEAD inhibitors for in vivo investigation against hepatocellular carcinoma. Eur J Med Chem. 2026;313:118886. [Content Brief]

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.

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MOQ

Minimum order quantity

100 mg

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

Produktname:
Art. -Nr.:
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LC-TD-05

Alle YAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

LC-TD-05 Related Classifications

HY-183753 Related Classifications