MRC-G-001
MRC-G-001 is a Genipin (HY-17389) derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.
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- Formel: C21H27NO4
- Molecular Weight:357.44
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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JAK1 |
STAT3 |
MRC-G-001 (Compound 2b) (0-500 μM,24-72 h) results in a dose- and time-dependent decrease in A549 cell viability, exhibiting stronger cytotoxicity compared to Genipin[1].
MRC-G-001 (0-100 μM, 7 days) can effectively inhibit the long-term proliferation ability of A549 cells[1].
MRC-G-001 (0-250 μM) strongly arrests the A549 cell cycle at the G1/S phase[1].
MRC-G-001 (0-250 μM, 24 h) promotes apoptosis to a greater extent than Genipin in A549 cells[1].
MRC-G-001 (0-250 μM, 24 h) effectively inhibits the EGFR and JAK1/STAT3 signaling pathway in A549 cells[1].
MRC-G-001 (100 μM, 0-24 h) suppresses the migration and invasion of A549 cells by interfering with TGF-β-induced EMT signaling pathway[1].
MRC-G-001 does not inhibit ATP-dependent EGFR kinase activity in A549 cells but binds to EGFR's extracellular domain (domain III), suggesting an alternative ATP-independent mechanism, likely by interfering with EGF binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0, 62.5, 125 and 250 μM
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Incubation Time:24 h
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Result:Decreased the phosphorylated p-Rb (Ser807/811) level.
Increased the level of cleaved caspase-3, cleaved caspase-8, and cleaved caspase-9.
Resulted in effective suppression of p-EGFR, p-JAK1, and p-STAT3 protein expression levels.
Did not alter UCP2 expression at lower concentrations, but slightly decreased its level at 250 μM.
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Cell Line:A549 cells
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Concentration:0, 62.5, 125 and 250 μM
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Incubation Time:24 h
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Result:Led to a dose-dependent increase in both early apoptotic and late apoptotic populations.
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Cell Line:A549 cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Led to an upregulation of E-cadherin and downregulation of N-cadherin, MMP9, Snail, and RhoA.
Inhibited the phosphorylation of SMAD2 and SMAD3, while SMAD4 protein levels remained largely unchanged.
Chemical Information
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Molecular Weight 357.44
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Formel C21H27NO4
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SMILES
[H][C@]12CC=C([C@]1([C@@H](OC=C2C(OC)=O)OC(C)C)[H])CNCC3=CC=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MRC-G-001 Related Classifications
HY-175009 Related Classifications
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