P-gp inhibitor 3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

P-gp inhibitor 3 

P-gp inhibitor 3 是一种高效的 P 糖蛋白 (P-gp) 抑制剂。P-gp inhibitor 3 通过激活 P-gp ATP 酶来抑制 P-gp 的外排功能。P-gp inhibitor 3 具有较强的多重耐药性 (MDR) 逆转能力，能增强紫杉醇抗肿瘤活性。

P-gp inhibitor 3

P-gp inhibitor 3 Chemical Structure

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生物活性

P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel[1].

IC50 & Target

P-glycoprotein
体外研究
(In Vitro)

P-gp inhibitor 3 (compound 16) (10 μM; 72 hours) has appreciable cytotoxicity in KBV cancer cells, with relatively stronger MDR reversal ability[1].
P-gp inhibitor 3 (2.5, 5, 10 μM ; 3 hours) reverses tumor MDR by inhibiting the efflux function of P-gp[1].
P-gp inhibitor 3 (0.25, 0.5, 1 mM; 5 minutes) can significantly increase ATP consumption in a concentration-dependent manner (p<0.01)[1].
P-gp inhibitor 3 (10 μM; 24 hours) induces apoptosis in KBV cells in the G2/M phase[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

Cell Line: KBV cells[1]
Concentration: 10 μM
Incubation Time: 72 hours
Result: Showed appreciable cytotoxicity in KBV cancer cells, and exhibited relatively stronger MDR reversal ability.

Cell Cycle Analysis

Cell Line: KBV cells[1]
Concentration: 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in KBV cells in the G2/M phase.

体内研究
(In Vivo)

P-gp inhibitor 3 (10 mg/kg; i.p., once a day, for 1 to 18 days) significantly enhances the anti-tumor activity of paclitaxel and the tumor suppression rate is 56.24%[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice xenograft tumor model (6-8 weeks old, BALB/c, male)[1]
Dosage: 10 mg/kg for P-gp inhibitor 3; 30 mg/kg for paclitaxel
Administration: i.p.; once a day (P-gp inhibitor 3), once every three days (paclitaxel); for 1 to 18 days
Result: Significantly enhanced the anti-tumor activity of paclitaxel and the tumor suppression rate was 56.24%.

分子量

782.06

Formula

C48H67N3O6
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.
参考文献

  • [1]. Huang W, et al. Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. Eur J Med Chem. 2022;232:114207.

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