2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Stem Cell/Wnt Epigenetics Apoptosis
  3. EGFR JAK STAT Apoptosis
  4. 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.

For research use only. We do not sell to patients.

MRC-G-001 Chemical Structure

MRC-G-001 Chemical Structure

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MRC-G-001 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target[1]

JAK1

 

STAT3

 

In Vitro

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.

MRC-G-001 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 62.5, 125 and 250 μM
Incubation Time: 24 h
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.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0, 62.5, 125 and 250 μM
Incubation Time: 24 h
Result: Led to a dose-dependent increase in both early apoptotic and late apoptotic populations.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 100 μM
Incubation Time: 24 h
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.
Molecular Weight

357.44

Formula

C21H27NO4
SMILES

[H][C@]12CC=C([C@]1([C@@H](OC=C2C(OC)=O)OC(C)C)[H])CNCC3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MRC-G-001 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRC-G-001EGFRJAKSTATApoptosisEpidermal growth factor receptorErbB-1HER1Janus kinaseGenipin derivativesA549 Cancer cellsInvasionMigrationEGFInhibitorinhibitorinhibit

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