Lonchocarpin
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- CAS 番号: 31501-55-0
- 分子式: C20H18O3
- 分子量:306.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW480 | IC50 |
4 nM
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Inhibitory activity against constitutive Wnt/β-catenin signaling in human SW480-pBAR/Renilla cells.
Inhibitory activity against constitutive Wnt/β-catenin signaling in human SW480-pBAR/Renilla cells.
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31817828 |
Lonchocarpin (5-20 μM) increases the protein (16 h) and mRNA (6 h) expression of HO-1, NQO1 and MnSOD in primary rat astrocytes[1].
Lonchocarpin (5-20 μM; 3 h) increases ARE nuclear protein binding and promotes Nrf2 nuclear translocation; it enhances ARE-mediated transcriptional activity (16 h)[1].
Lonchocarpin (5-20 μM; 1 h) increases the phosphorylation of AMPK, ERK1/2, JNK and p38 MAPK[1].
Lonchocarpine (20 μM; 16 h) induces the expression of HO-1 in primary rat astrocytes. This process is positively regulated by AMPK and JNK, negatively regulated by p38 MAPK, and unaffected by ERK[1].
Pretreatment of primary rat astrocytes with lonchocarpin (5-20 μM) for 1 h followed by exposure to H2O2 (50 μM) reduces H2O2-induced intracellular ROS levels and attenuates H2O2-caused decrease in cell viability[1].
ARE-mediated transcriptional activity induced by lonchocarpine (20 μM) in primary rat astrocytes is positively regulated by AMPK and JNK, negatively regulated by p38 MAPK, and unaffected by ERK[1].
Lonchocarpine (20 μM)-induced binding of nuclear proteins to ARE in primary rat astrocytes is positively regulated by AMPK and JNK, and negatively regulated by p38 MAPK[1].
Lonchocarpin (1-30 μM; 24 h) inhibits Wnt/β-catenin reporter activity in a concentration-dependent manner in RKO and SW480 cells, with an IC50 of 4 μM in SW480 pBAR/Renilla cells. Lonchocarpin also reduces nuclear β-catenin levels without significantly decreasing total β-catenin, and inhibits Wnt/β-catenin signaling driven by wild-type β-catenin, constitutively active β-catenin S33A, or dnTCF4-VP16, supporting that it acts downstream of β-catenin stabilization and suppresses TCF-mediated transcription[2].
Lonchocarpin (5-20 μM; 24 h) inhibits the proliferation of HCT116, SW480 and DLD-1 colorectal cancer cells. Specifically, 10 μM and 20 μM of lonchocarpin reduce the number of EdU-positive SW480 cells by 50% and 85%, respectively, and decrease the number of EdU-positive DLD-1 cells by 40% and 75%, while exerting no significant effect on the proliferation of non-tumorigenic IEC-6 cells[2].
Lonchocarpin (5-20 μM; 24 h) inhibits migration of HCT116, SW480 and DLD-1 cells; at 20 μM, it reduces scratch closure by 55%, 55% and 45% in HCT116, SW480 and DLD-1 cells respectively, and reduces scratch closure by 40% in SW480 cells at 10 μM, but does not significantly affect migration of IEC-6 cells[2].
Lonchocarpin (20-50 μM) also preferentially reduces the MTT viability signal of colorectal cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RKO human colorectal cancer cells
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Concentration:10, 20 µM
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Incubation Time:24 h
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Result:Reduced Wnt3a-induced nuclear β-catenin-positive cells from 86% to 54% at 10 µM and to 30% at 20 µM.
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Cell Line:RKO human colorectal cancer cells
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Concentration:20 µM
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Incubation Time:overnight
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Result:Did not significantly reduce total β-catenin protein levels, but reduced β-catenin levels in the nuclear fraction, with corresponding changes in cytosolic β-catenin levels.
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Cell Line:HCT116, SW480, DLD-1 human colorectal cancer cells, IEC-6 non-tumoral rat intestinal cells
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Concentration:5, 10, 20, 30 µM
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Incubation Time:24 h
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Result:Inhibited 33% of EdU-positive HCT116 cells at 5 and 10 µM, and 75% at 30 µM.
Inhibited 50% of EdU-positive SW480 cells at 10 µM and 85% at 20 µM.
Inhibited 40% of EdU-positive DLD-1 cells at 10 µM and 75% at 20 µM.
Showed no effect on EdU-positive IEC-6 cell count at 5, 10, or 20 µM.
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Cell Line:HCT116, SW480, DLD-1 human colorectal cancer cells, IEC-6 non-tumoral rat intestinal cells
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Concentration:10, 20, 30, 40, 50 µM
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Incubation Time:24 h; 48 h; 72 h
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Result:Reduced absorbance in HCT116, SW480, and DLD-1 cells at 20-50 µM across all time points, while 10 µM had no effect.
Reduced absorbance in IEC-6 cells only at 50 µM across all time points, and at 40 µM only at 72 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female 129SvJxC57BL6 mixed mice, 8-12 weeks old, AOM/DSS-induced colorectal adenocarcinoma model[2]
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Dosage:50 mg/kg; 100 mg/kg/day
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Administration:i.p.; daily; 4 days; split into two 50 mg/kg doses every 12 hours (100 mg/kg/day group)
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Result:Reduced Ki-67-positive cells in adenocarcinomas by 31% compared to vehicle control.
Reduced BrdU-positive cells in adenocarcinomas by 38% compared to vehicle control.
Showed no statistically significant antiproliferative effects at 50 mg/kg/day dose.
化学情報
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CAS 番号 31501-55-0
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分子量 306.36
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分子式 C20H18O3
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SMILES
O=C(/C=C/C1=CC=CC=C1)C2=CC=C3C(C=CC(C)(O3)C)=C2O
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別名
Lonchocarpine
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Structure Classification
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Initial Source
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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)