1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp-IN-32

P-gp-IN-32 是一种 P-糖蛋白 (P-gp) 抑制剂。P-gp-IN-32 具有低细胞毒性,并且在 MCF7/ADR 细胞中对 Doxorubicin (HY-15142A) 表现出强效的多药耐药 (MDR) 逆转活性 (IC50 值为 0.11 μM, 耐药逆转倍数 (RF) 值为 215.9)。P-gp-IN-32 可直接与 P-gp 结合,诱导 P-gp 的构象变化并抑制其外排功能。P-gp-IN-32 可用于癌症研究,如乳腺癌。

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P-gp-IN-32

P-gp-IN-32 Chemical Structure

CAS No. : 2918249-59-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer[1].

体外研究
(In Vitro)

P-gp-IN-32 (Compound BP3p) (5 μM) 在 MCF-7 和 MCF-7/ADR 细胞中均显示出低于 25% 的生长抑制率[1]。 P-gp-IN-32 在 MCF-7/ADR 细胞中,与 Doxorubicin (HY-15142A) 联合使用时,Doxorubicin的 IC50 值为 0.11 μM,耐药逆转倍数为 215.9[1]
P-gp-IN-32 (2.5-5 μM, 4 h) 以剂量依赖性方式增加 MCF-7/ADR 细胞中罗丹明 123 的积累[1]
P-gp-IN-32 (0.5-5 μM, 48 h) 对 MCF-7/ADR 细胞中 P-gp 的表达无显著影响[1]
P-gp-IN-32 (50 μM) 可增强 MCF-7/ADR 细胞中 UIC-2 抗体 (HY-P990196) 与 P-gp 的结合[1]
P-gp-IN-32 (5 μM, 5 days) 与阿霉素联合使用时,可减小 MCF-7/ADR 三维肿瘤球状体的体积[1]

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

Western Blot Analysis[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.5, 2.5 and 5 μM
Incubation Time: 48 h
Result: Did not reduce P-gp expression.
分子量

562.65

Formula

C35H34N2O5

CAS 号
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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产品名称:
P-gp-IN-32
目录号:
HY-175838
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