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.
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- Formule: C27H23F3N4O2
- Masse moléculaire:492.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Activité biologique
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TEAD4 68.3 nM (IC50) |
TEAD1 116.6 nM (IC50) |
TEAD2 168.7 nM (IC50) |
TEAD3 1261.0 nM (IC50) |
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.
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Cell Line:HCC LM3 cells
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Concentration:3 μM
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Incubation Time:10-14 days
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Result:Significantly reduced the number of colonies formed by HCC LM3 cells compared to DMSO control.
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Cell Line:HCC LM3 cells
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Concentration:0.3, 1, 3 and 10 μM
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Incubation Time:3 hours
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Result:Significantly downregulated the mRNA expression of CTGF and CYR61 in a dose-dependent manner, with maximal suppression at 10 μM.
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Cell Line:HCC LM3 cells
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Concentration:3 and 10 μM
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Incubation Time:72 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 4-6 weeks old)[1]
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Dosage:50 mg/kg
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Administration:i.p.; once daily; 17 days
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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
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Masse moléculaire 492.49
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Formule C27H23F3N4O2
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SMILES
O=C(N1CCN(C(C2=CC=CC3=C2C=CN3C4=CC=C(C(F)(F)F)C=C4)=O)CC1)NC5=CC=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LC-TD-05 Related Classifications
HY-183753 Related Classifications
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