2. Membrane Transporter/Ion Channel Apoptosis
  3. P-glycoprotein Apoptosis
  4. ABCB1-IN-3

ABCB1-IN-3 (Compound K27) 是一种有口服活性的 ABCB1 抑制剂，可诱导细胞凋亡 (apoptosis)。ABCB1-IN-3 直接与 ABCB1 结合，抑制外排功能，保证细胞内紫杉醇 (Paclitaxel) (HY-B0015) 浓度稳定，而不影响 ABCB1 的正常表达。BCB1-IN-3 在体外显著增加 ABCB1 介导的多药耐药 (MDR) 对 Paclitaxel 的敏感性，导致细胞周期阻滞，抑制细胞增殖。BCB1-IN-3 与 Paclitaxel 联合使用在体内表现出强大的肿瘤抑制作用，且不产生毒性。

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ABCB1-IN-3 Chemical Structure

ABCB1-IN-3 Chemical Structure

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ABCB1-IN-3 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

ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity[1].

体外研究
(In Vitro)

ABCB1-IN-3 (72 小时) 显著提高 ABCB1 介导的 MDR SW620/AD300 细胞对 Paclitaxel 的敏感性 (IC50=15.33nM)，单独使用时即使在 20 μM 的高浓度下也几乎无毒性[1]。
ABCB1-IN-3 (5-20 μM; 24 小时) 明显增强 Paclitaxel 对 SW620/AD300 细胞周期的阻滞作用，从而抑制其增殖[1]。
ABCB1-IN-3 (5-20 μM; 7天) 与 Paclitaxel 联用可抑制细胞集落形成，对 Paclitaxel 耐药细胞表现出很强的逆转活性[1]。
ABCB1-IN-3 (5-20 μM; 24 小时) 被证实可直接与 ABCB1 结合抑制外排功能，减少细胞外排，保证 Paclitaxel 细胞内浓度稳定，而不影响 ABCB1 的正常表达[1]。

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

ABCB1-IN-3 相关抗体:

Cell Cycle Analysis[1]

Cell Line: SW620/AD300 cells
Concentration: 5, 10, 20 μM
Incubation Time: 24 h
Result: Induced more cells to stay in the G2/M phase combined with Paclitaxel.

Cell Proliferation Assay[1]

Cell Line: SW620/AD300 cells
Concentration: 5, 10, 20 μM
Incubation Time: 7 days
Result: Significantly inhibited the cell colony formation of SW620/AD300 cells combined with Paclitaxel.
体内研究
(In Vivo)

ABCB1-IN-3 (50 mg/kg; 灌胃；3 天给药一次，持续 14 天) 与 Paclitaxel 联合使用时，在接种 SW620/AD300 细胞的雄性 BALB/c 裸鼠中表现出强效的肿瘤抑制作用，且不产生毒性，但单独使用时肿瘤抑制作用较弱[1]。

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

Animal Model: Male BALB/c nude mice (18-22 g, aged 6-7 weeks, 1×107 SW620/AD300 cells were inoculated subcutaneously into the forelimb of each mouse.)[1]
Dosage: 50 mg/kg
Administration: Intragastric gavage (i.g.); once every 3 days for 14 days
Result: The tumor volume and weight had little difference when used alone, and remarkable reduced when combined with Paclitaxel, showing better antitumor activity.
The cell apoptosis in tumor tissues was more remarkable when used with Paclitaxel, resulted in more massive degeneration and necrosis than in vehicle or mono-therapy groups.
Showed no significant loss of body weight.
分子量

288.34

Formula

C19H16N2O
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

ABCB1-IN-3 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:

ABCB1-IN-3P-glycoproteinApoptosisP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243apoptosisABCB1 inhibitoranti-tumormultidrug resistanceMDRInhibitorinhibitorinhibit

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