7,3′,4′-Trihydroxyisoflavone 是黄豆苷元的主要代谢物,是 Cot (Tpl2/MAP3K8) 和 MKK4 的 ATP 竞争性抑制剂。7,3′,4′-Trihydroxyisoflavone 具有抗癌、抗血管生成、化学保护和自由基清除活性。
7,3′,4′-Trihydroxyisoflavone Chemical Structure
CAS No. : 485-63-2
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
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生物活性
7,3′,4′-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3′,4′-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities[1][2].
体外研究 (In Vitro)
7,3′,4′-Trihydroxyisoflavone triggers cell cycle arrest at the G1 phase and displays an anti-proliferative effect against EGF receptor-positive skin cancer[1]. 7,3′,4′-Trihydroxyisoflavone also significantly inhibits UVB-induced COX-2 expression by suppressing the NF-B transcription activity in mouse skin epidermal JB6 P+ cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
In a mouse skin tumorigenesis model, 7,3′,4′-Trihydroxyisoflavone strongly suppresses the incidence, multiplicity, and volume of UVB-induced mouse skin tumors. Consistent with the tumor data, 7,3′,4′-Trihydroxyisoflavone clearly attenuates UVB-induced COX-2 expression in hairless mouse skin[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
270.24
Formula
C15H10O5
CAS 号
485-63-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yu-Li Lo, et al. 7,3′,4′-Trihydroxyisoflavone modulates multidrug resistance transporters and induces apoptosis via production of reactive oxygen species. Toxicology. 2012 Dec 16;302(2-3):221-32.
[2]. Dong Eun Lee, et al. 7,3′,4′-Trihydroxyisoflavone, a metabolite of the soy isoflavone daidzein, suppresses ultraviolet B-induced skin cancer by targeting Cot and MKK4. J Biol Chem. 2011 Apr 22;286(16):14246-56.
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
体外研究 (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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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.
体内研究 (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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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.
分子量
270.24
Formula
C15H10O5
CAS 号
17817-31-1
中文名称
4′,6,7-三羟基异黄酮
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lee DE, et al. 6,7,4′-trihydroxyisoflavone inhibits HCT-116 human colon cancer cell proliferation by targeting CDK1 and CDK2. Carcinogenesis. 2011 Apr;32(4):629-35.
[2]. Lim TG, et al. The daidzein metabolite, 6,7,4′-Trihydroxyisoflavone, is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1. Int J Mol Sci. 2014 Nov 19;15(11):21419-32
[3]. Seo SG, et al. A metabolite of daidzein, 6,7,4′-trihydroxyisoflavone, suppresses adipogenesis in 3T3-L1 preadipocytes via ATP-competitive inhibition of PI3K.