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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C27H23F3N4O2
- 分子量:492.49
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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.
化学情報
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分子量 492.49
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
LC-TD-05 関連分類
HY-183753 関連分類
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