2. Membrane Transporter/Ion Channel Apoptosis Autophagy
  3. P-glycoprotein Apoptosis Autophagy
  4. P-gp inhibitor 30

P-gp inhibitor 30 是一种强效的 P-gp 抑制剂，能逆转乳腺癌的多药耐药性，使耐药细胞对 Doxorubicin (ADM) (HY-15142) 敏感。P-gp inhibitor 30 与 ADM 联合使用时，可促进耐药乳腺癌细胞细胞凋亡 (apoptosis)，诱导自噬 (autophagy)，抑制细胞增殖、迁移和侵袭。P-gp inhibitor 30 在体外和体内均能抑制乳腺癌肿瘤生长。P-gp inhibitor 30 可用于耐药性乳腺癌的相关研究。

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P-gp inhibitor 30

P-gp inhibitor 30 Chemical Structure

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P-gp inhibitor 30 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis , induces autophagy,and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research[1].

体外研究
(In Vitro)

P-gp inhibitor 30 (compound A38) (0.1 μM) 可逆转 MDA-MB-231/ADM 细胞的 ADM 耐药性，显著降低 ADM 的 IC50 值，从 785.46 μM 降至 2.05 μM[1]。
P-gp inhibitor 30 (0.125-4 μM) 以浓度依赖的方式显著抑制不同浓度下的 P-gp ATPase 活性[1]。
P-gp inhibitor 30 与 P-gp 相互作用，抑制其功能而不下调其表达，并稳定该蛋白，从而在升温条件下减少其在 MCF7/ADM 细胞中的降解[1]。
P-gp inhibitor 30 (6 h) 可显著增加 MCF7/ADM 细胞中 Rh123 的表达强度，并增加 MDA-MB-231/ADM 细胞中 ADM 的积累，同时抑制 Rh123 的外排[1]。
P-gp inhibitor 30 (0.1-1 μM，24 小时 -15 天) 与 ADM 联用时，可促进乳腺癌耐药细胞 (MCF7/ADM 和 MDA-MB-231/ADM 细胞) 的凋亡，抑制细胞增殖，迁移和侵袭，表明其可增强这些细胞对 ADM 的敏感性[1]。
P-gp inhibitor 30 (0.1 μM) 与 ADM 联用时，可导致 MCF7/ADM 和 MDA-MB-231/ADM 细胞中自噬体的积累，并显著增加自噬相关蛋白的表达，从而诱导细胞死亡[1]。
P-gp inhibitor 30 (1-10 天) 与 ADM 联用时，在 3D 肿瘤球体模型中可显著缩小 MCF7/ADM 和 MDA-MB-231/ADM 细胞的肿瘤体积[1]。

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

P-gp inhibitor 30 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF7/ADM and MDA-MB-231/ADM cells
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Significantly increases the expression level of LC3 when combined with ADM.

Apoptosis Analysis[1]

Cell Line: MCF7/ADM and MDA-MB-231/ADM cells
Concentration: 0.1, 0.5 and 1 μM
Incubation Time: 48 h
Result: Significantly increased ADM-induced apoptosis in a dose-dependent manner compared to the MCF7/ADM control group.
Significantly increased ADM-induced apoptosis on MDA-MB-231/ADM cells.

Cell Proliferation Assay[1]

Cell Line: MCF7/ADM and MDA-MB-231/ADM cells
Concentration: 0.1, 0.5 and 1 μM
Incubation Time: 15 days
Result: Significantly inhibited the proliferation of MCF7/ADM cells in a dose-dependent manner compared to the MCF7/ ADM control group when combined with ADM.
Resulted in only a few cells survived at a concentration of 1 μM.
Markedly inhibited the proliferation of drug-resistant breast cancer cells when combined with ADM.

Cell Migration Assay [1]

Cell Line: MCF7/ADM and MDA-MB-231/ADM cells
Concentration: 0.1 μM
Incubation Time: 36 h
Result: Suppressed the migration ability of breast cancer drug- resistant cells when combined with ADM.

Cell Invasion Assay[1]

Cell Line: MCF7/ADM and MDA-MB-231/ADM cells
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Suppressed the invasion ability of breast cancer drug- resistant cells when combined with ADM.
体内研究
(In Vivo)

P-gp inhibitor 30 (2 mg/kg，腹腔注射，每 2 天一次，持续 14 天) 与 ADM 联合使用时，在 MCF-7/ADM 小鼠模型中显示出抗肿瘤作用[1]。

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

Animal Model: Female BALB/c nude mice (4-5 weeks old) subcutaneously injected with MCF-7/ADM cells[1]
Dosage: 2 mg/kg
Administration: i.p., every 2 days for 14 days
Result: Significantly reduced tumor size when combined with ADM (10 mg/kg), with efficacy comparable to Tariquidar (HY-10550).
Showed significantly lower tumor weight than that of other groups.
Showed no significant loss compared to control.
Caused no significant tissue cell necrosis.
分子量

386.38

Formula

C22H15FN4O2
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

P-gp inhibitor 30 相关分类

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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.

Keywords:

P-gp inhibitor 30P-glycoproteinApoptosisAutophagyP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243drug-resistant breast cancerADMMCF7/ADMMDA-MB-231/ADMInhibitorinhibitorinhibit

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