2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Hapalosin

Hapalosin 是一种多药耐药逆转剂和化学增敏剂，对癌细胞具有轻度细胞毒性。Hapalosin 可抑制 P-糖蛋白 (P-glycoprotein) 的 ATP 依赖性药物外排泵功能，并拮抗多药耐药相关蛋白。Hapalosin 可逆转由 P-糖蛋白和多药耐药相关蛋白介导的多药耐药性，增加经 P-糖蛋白转运的药物在细胞内的蓄积，并增强这些药物对过表达 P-糖蛋白的癌细胞的细胞毒性。Hapalosin 可用于多药耐药性癌症的研究。

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Hapalosin

Hapalosin Chemical Structure

CAS No. : 159542-04-8

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Hapalosin 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

Hapalosin is a multidrug resistance reversal agent and chemosensitizer with mild cytotoxicity against cancer cells. Hapalosin inhibits the ATP-dependent drug efflux pump function of P-glycoprotein and antagonizes multidrug resistance-associated proteins. Hapalosin reverses multidrug resistance mediated by P-glycoprotein and multidrug resistance-associated proteins, increases the intracellular accumulation of drugs transported by P-glycoprotein, and enhances the cytotoxicity of these drugs against cancer cells overexpressing P-glycoprotein. Hapalosin can be used in the research of multidrug-resistant cancers[1][2].

体外研究
(In Vitro)

Hapalosin (1-6 µg/mL; 48 h) 可逆转 MCF-7/ADR 细胞中由 P-gp 介导的多药耐药 (MDR)，其 EC50 为 1 µg/mL；同时该化合物对这些细胞的固有细胞毒性的 IC20 为 6 µg/mL[1]。
Hapalosin (0.7-6 µg/mL; 48 h) 可逆转 HL-60/ADR 细胞中由 MRP 介导的多药耐药 (MDR)，其 EC50 为 0.7 µg/mL；同时该药物对这些细胞的固有细胞毒性的 IC20 为 6 µg/mL[1]。
Hapalosin (60 min) 可有效提高 MCF-7/ADR 细胞内 [3H]-Vinblastine (HY-13780) 的积累量，表明其可抑制 P-gp 介导的药物外排[1]。
Hapalosin (20 μM; 90 min) 可通过抑制 P-糖蛋白外排泵，增加 SKVLB1 细胞内 [3H]-Vinblastine 和 [3H]-Paclitaxel (HY-B0015) 的积累；在 20 μM 浓度下，[3H]-Paclitaxel 的积累量较对照组提升 440%，且该物质不影响 SKOV3 细胞内的药物积累[2]。
Hapalosin (2.5-12.5 μM; 48 h) 在浓度 ≥ 2.5 μM 时可选择性增强经 P-糖蛋白转运的化疗药物对 MCF-7/ADR 细胞的细胞毒性，且在 5 μM 浓度下可完全逆转这些细胞中由 P-糖蛋白介导的对长春碱的多药耐药性[2]。
Hapalosin 对 KB、LoVo 和 MCF-7/ADR 细胞具有细胞毒性，其 IC50 值分别为 2.5 μg/mL、2 μg/mL 和 5-15 μM[2]。

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

Hapalosin 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7/ADR (P-gp-overexpressing, MRP-negative breast carcinoma cells)
Concentration: 6 µg/mL (alone); 1 µg/mL (in presence of 25 nM actinomycin D)
Incubation Time: 48 h
Result: Exhibited an IC20 of 6 µg/mL for intrinsic cytotoxicity.
Exhibited an EC50 of 1 µg/mL for reversing P-gp-mediated MDR in the presence of actinomycin D.
Was more effective at reversing P-gp-mediated MDR than all tested D-glucose mimetics of hapalosin.

Cell Cytotoxicity Assay[1]

Cell Line: HL-60/ADR (MRP-expressing, P-gp-negative promyelocytic leukemia cells)
Concentration: 6 µg/mL (alone); 0.7 µg/mL (in presence of 2 nM vincristine)
Incubation Time: 48 h
Result: Exhibited an IC20 of 6 µg/mL for intrinsic cytotoxicity.
Exhibited an EC50 of 0.7 µg/mL for reversing MRP-mediated MDR in the presence of vincristine.
Showed similar efficacy in reversing MRP-mediated MDR to select D-glucose mimetics.
分子量

489.64

Formula

C28H43NO6
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

Hapalosin 相关分类

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  • 稀释计算器

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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:

Hapalosin159542-04-8P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243human nasopharyngeal carcinomaHL-60/ADR cellsmultidrug resistance-associated proteinSKVLB1 cellshuman colon adenocarcinoma cellsmultidrug resistanceSKOV3 cellsMCF-7/ADR cellscancer cellsInhibitorinhibitorinhibit

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