2. Apoptosis
  3. Apoptosis Caspase
  4. 4′-O-Methylglabridin

4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases.

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4′-O-Methylglabridin

4′-O-Methylglabridin Chemical Structure

CAS No. : 68978-09-6

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4′-O-Methylglabridin Related Antibodies

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Description

4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases[1][2].

IC50 & Target[1]

Caspase-9

 

In Vitro

4′-O-Methylglabridin (2.5-40 μM; 72 h) inhibits proliferation of Huh7, MCF7, and HCT116 cancer cell lines in vitro, with the strongest activity against Huh7 cells (IC50=9.6 μM)[1].
4′-O-Methylglabridin (IC50 concentration; 24 h, 48 h, 72 h) inhibits proliferation of Huh7 cells in a time-dependent manner, with IC50 values increasing from 7.31 μM at 24 h to 11.4 μM at 72 h[1].
4′-O-Methylglabridin (10 μM; 48 h) induces apoptotic nuclear changes in Huh7 cells after 48 h of treatment[1].
4′-O-Methylglabridin (10 μM; 48 h) induces caspase-dependent apoptosis in Huh7 cells after 48 h of treatment by increasing cytochrome C release and cleaved caspase-9 levels, while also reducing phospho-Rb, p53, Mdm2, and p21 levels to disrupt cell cycle regulation[1].
4′-O-Methylglabridin (50 μM; 90 min at 50°C) inhibits β-carotene consumption by 78% in a cell-free β-carotene-linoleate assay[2].
4′-O-Methylglabridin (30 μM; 2 h at 37°C) potently inhibits AAPH-induced oxidation of ex vivo human LDL[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

4′-O-Methylglabridin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Huh7, MCF7, HCT116
Concentration: 2.5, 5, 10, 20, 40 μM
Incubation Time: 72 h
Result: Inhibited proliferation of Huh7 cells with an IC50 of 9.6 μM.
Inhibited proliferation of MCF7 cells with an IC50 of 16.5 μM.
Inhibited proliferation of HCT116 cells with an IC50 of 10.8 μM.

Cell Proliferation Assay[1]

Cell Line: Huh7
Concentration: IC50 concentration Test
Incubation Time: 24 h, 48 h, 72 h (monitored every 10 min for first 24 h, then every 30 min for remaining 48 h)
Result: Inhibited Huh7 cell proliferation with an IC50 of 7.31 μM at 24 h.
Inhibited Huh7 cell proliferation with an IC50 of 9.8 μM at 48 h.
Inhibited Huh7 cell proliferation with an IC50 of 11.4 μM at 72 h.

Apoptosis Analysis[1]

Cell Line: Huh7
Concentration: 10 μM
Incubation Time: 48 h
Result: Increased the percentage of Huh7 cells in the subG1 phase to 5.26% relative to DMSO control.
Induced accumulation of Huh7 cells in the G2/M phase to 20.32% relative to DMSO control.
Induced changes in Huh7 cell nuclei consistent with apoptotic cell death, as detected by Hoechst staining.

Western Blot Analysis[1]

Cell Line: Huh7
Concentration: 10 μM (48 h IC50)
Incubation Time: 48 h
Result: Increased cytochrome C and cleaved caspase-9 protein levels relative to DMSO control.
Decreased phospho-Rb (Ser807/811), p53, Mdm2, and p21 protein levels relative to DMSO control.
Did not increase cleaved PARP protein levels relative to DMSO control.
Molecular Weight

338.40

Formula

C21H22O4
CAS No.
SMILES

CC1(OC2=C(C=C1)C3=C(C=C2)C[C@H](C4=C(C=C(C=C4)OC)O)CO3)C
Structure Classification
Initial Source
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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4′-O-Methylglabridin 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:

4′-O-Methylglabridin68978-09-6ApoptosisCaspasep21phospho-Rb (Ser807/811)cell cycleMCF7breast cancer cell linescolorectal cancer cell linesapoptosishepatocellular cancer cell linesHCT116Huh7Inhibitorinhibitorinhibit

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