2. Membrane Transporter/Ion Channel Stem Cell/Wnt JAK/STAT Signaling
  3. P-glycoprotein STAT
  4. P-gp-IN-36

P-gp-IN-36 是一种强效的 P-糖蛋白 (P-gp) 抑制剂，其 EC50 约为 1 μM。P-gp-IN-36 可抑制 P-糖蛋白的外排功能，逆转癌细胞中由 P-gp 介导的多药耐药性。P-gp-IN-36 可抑制 STAT3 的磷酸化并降低总 STAT3 的表达水平。P-gp-IN-36 可使表达 P-gp 的癌细胞对常规细胞抑制药物的细胞抑制作用增敏。P-gp-IN-36 可用于多药耐药性癌症的研究。

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P-gp-IN-36

P-gp-IN-36 Chemical Structure

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P-gp-IN-36 相关抗体

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. P-gp-IN-36 inhibits the efflux function of P-glycoprotein, overcoming P-gp-mediated multidrug resistance in cancer cells. P-gp-IN-36 inhibits STAT3 phosphorylation and reduces total STAT3 expression. P-gp-IN-36 sensitizes P-gp-expressing cancer cells to the cytostatic effects of conventional cytostatic drugs. P-gp-IN-36 can be used for the research of multidrug-resistant cancer[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

P-gp-IN-36 (LD) (0.25-64 μM; 30 min) 可强效抑制 P388/MDR 细胞中的 P-gp，其 EC50 约为 1 μM[1]。
P-gp-IN-36 (0.25-64 μM; 30 min) 可强效抑制 CT26 细胞中的 P-gp，即便该细胞系本身的 P-gp 表达水平较低[1]。
P-gp-IN-36 (15 h) 可通过降低 STAT3 磷酸化水平及总 STAT3 蛋白表达，强效抑制 CT26 细胞中的 STAT3 信号通路[1]。
P-gp-IN-36 (0.5-2 μM; 72 h) 可强效使 P388/MDR 细胞对 Doxorubicin (HY-15142A) 的细胞抑制作用增敏，在 2 μM 浓度下可使 Doxorubicin 的 IC50 降低约 86 倍[1]。
P-gp-IN-36 (1-4 μM; 48 h) 可显著增强 Doxorubicin 诱导的 P388/MDR 细胞凋亡，并以浓度依赖的方式降低活细胞群数量[1]。
P-gp-IN-36 (2 μM; 48 h) 可通过在 2 μM 浓度下显著提升 caspase-3 活性，增强 Doxorubicin 诱导的 P388/MDR 细胞凋亡[1]。

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

P-gp-IN-36 相关抗体:

Cell Proliferation Assay[1]

Cell Line: P388/MDR mouse monocytic leukemia cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 72 h
Result: Reduced the IC50 of DOX from 8.62 μM (without LD) to 2.29 μM (with 0.5 μM LD), 0.36 μM (with 1 μM LD), and 0.10 μM (with 2 μM LD).
Corresponding to an ~86-fold reduction in DOX IC50 at the highest tested LD concentration.

Apoptosis Analysis[1]

Cell Line: P388/MDR mouse monocytic leukemia cells
Concentration: 1, 2, 4 μM
Incubation Time: 48 h
Result: Decreased the percentage of live cells from 85% (DOX alone) to 68% (DOX + 1 μM LD).
Induced nearly complete apoptosis at 4 μM LD, with the live cell fraction further reduced.
分子量

754.95

Formula

C44H58N4O7
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-IN-36 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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-IN-36P-glycoproteinSTATP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243multidrug-resistant cancerSTAT3 phosphorylationCT26 cellsapoptosisP388/MDR cellscancer cellscaspase-3STAT3 signalingmultidrug resistanceInhibitorinhibitorinhibit

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