1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. 8α,9α-Epoxycoleon-U-quinone

8α,9α-Epoxycoleon-U-quinone 

目录号: HY-N10564
产品使用指南

8α,9α-Epoxycoleon-U-quinone (化合物 3) 是一种对癌细胞具有选择性 (SI=2.0) 的 p-糖蛋白 (P-gp) 调节剂。8α,9α-Epoxycoleon-U-quinone 能有效抑制 NCI-H460/R 细胞中的 P-gp 活性,并在与 Doxorubicin (DOX) (HY-15142A) 联合后,逆转癌细胞对 DOX 的抗性,增强 DOX 的抗癌效果。

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8α,9α-Epoxycoleon-U-quinone Chemical Structure

8α,9α-Epoxycoleon-U-quinone Chemical Structure

CAS No. : 93800-59-0

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  • 生物活性

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  • 参考文献

生物活性

8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX[1].

体外研究
(In Vitro)

8α,9α-Epoxycoleon-U-quinone (2, 5, 10, 20, 50 μM; 72 h) selective towards cancer cell lines, with a selectivity index of 2.0[1].
8α,9α-Epoxycoleon-U-quinone (10 μM; 72 h) is able to inhibit P-glycoprotein (P-gp) activity in NCI-H460/R cells[1].
8α,9α-Epoxycoleon-U-quinone (1, 2, 5 μM; 72 h) reverses the resistance of cancer cells to DOX and increase anti-cancer efficacy of DOX[1].

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

Cell Viability Assay[1]

Cell Line: NCI-H460, NCI-H460/R, MRC-5 cells
Concentration: 2, 5, 10, 20, 50 μM
Incubation Time: 72 h
Result: Showed inhibition of cancer cell viability (IC50≈20 μM) with a selectivity index of 2.0.

Cell Viability Assay[1]

Cell Line: NCI-H460/R cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Decreased the Rho123 accumulation in NCI-H460/R cells, and no influence on the ABCB1 expression.

Cell Viability Assay[1]

Cell Line: NCI-H460/R cells
Concentration: 1, 2, 5 μM (combine with Doxorubicin (DOX))
Incubation Time: 72 h (pre-treat)
Result: Promoted sensitization of NCI-H4l60/R cells to DOX with relative reversal indexes of 1.976 and 4.696 for concentration of 1 and 2 μM, respectively.
分子量

360.40

Formula

C20H24O6

CAS 号
结构分类
初始来源
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.

纯度 & 产品资料
参考文献
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  • 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.

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