1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
    Epigenetics
    TGF-beta/Smad
  2. CDK
    PI3K
    PKC
  3. Desmethylglycitein

Desmethylglycitein (Synonyms: 4',6,7-Trihydroxyisoflavone)

Cat. No.: HY-N5072
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Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.

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Desmethylglycitein Chemical Structure

Desmethylglycitein Chemical Structure

CAS No. : 17817-31-1

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Description

Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity[1]. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1)[2]. Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes[3].

IC50 & Target[1][2][3]

CDK1

 

CDK2

 

PKC

 

In Vitro

Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppesses anchorage-dependent growth of HCT-116 and DLD1 cells in a dose- and time-dependent manner without cytotoxicity [1].
Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppresses CDK1 activity in a dose-dependent manner and inhibits CDK2 activity in HCT-116 cells[1].
Desmethylglycitein (4',6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) induces cell cycle arrest at the S and G2/M phases, the percentage of cells in S phase is higher in the 100 μM 6,7,4′-THIF-treated group, and the same pattern is observed in G2/M phase (29.5% versus 19.1% ) [1].

Cell Viability Assay[1]

Cell Line: HCT-116 cells
Concentration: 0, 12.5, 25, 50 or 100 μM
Incubation Time: 24, 48 or 72 hours
Result: Inhibited anchorage-dependent and -independent growth of HCT-116 cells.

Western Blot Analysis[1]

Cell Line: HCT-116 and DLD1 cells
Concentration: 0, 25, 50 or 100 μM
Incubation Time: 48 hours
Result: Inhibited CDK1,CDK2 expression.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0, 25, 50 or 100 μM
Incubation Time: 24, 48 or 72 hours
Result: Induces cell cycle arrest of HCT-116 cells at S and G2/M phases.
In Vivo

Desmethylglycitein (4',6,7-Trihydroxyisoflavone) (intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days) suppresses tumor development in mice and serves as an effective anticancer treatment with the potential to inhibit or delay the tumorigenicity of HCT-116 cells in an in vivo system[1].

Animal Model: Female athymic nude mice subcutaneously injected with HCT-116 cells[1]
Dosage: 5 or 25 mg/kg
Administration: Intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days
Result: Decreased tumor growth, volume and weight of HCT-116 xenografts.
Molecular Weight

270.24

Formula

C₁₅H₁₀O₅

CAS No.

17817-31-1

SMILES

O=C1C(C2=CC=C(O)C=C2)=COC3=CC(O)=C(O)C=C13

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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