2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. P-gp inhibitor 5

P-gp inhibitor 5 是一种有效的 P 糖蛋白 (P-gp) 抑制剂。P-gp inhibitor 5 对某些癌细胞有抗增殖活性。P-gp inhibitor 5 可通过恢复细胞对长春新碱 (Vincristine; HY-N0488A) 和紫杉醇 (Paclitaxel; HY-B0015) 的敏感性，有效逆转 ABCB1/Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。

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P-gp inhibitor 5 Chemical Structure

P-gp inhibitor 5 Chemical Structure

CAS No. : 2451298-06-7

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P-gp inhibitor 5 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 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015)[1].

IC50 & Target

P-gp[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Flp-In-293 IC50
> 40 μM
Compound: 10
Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 32569926]
Flp-In-293 IC50
29.7 μM
Compound: 10
Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 32569926]
HeLa IC50
> 40 μM
Compound: 10
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 32569926]
体外研究
(In Vitro)

P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-InTM-293 and KBvin cells with IC50s of 29.7 and 12.6 μM, respectively[1].
P-gp inhibitor 5 (2.5 and 5 μM) lows the IC50s of KBvin cells for Vincristine to 7.59~36.82 nM, for Paclitaxel to 21.0~79.5 nM, for Doxorubicin to 85.7~111 nM; lows the IC50s of HeLaS3 cells for Vincristine to 2.24~3.91 nM, for Paclitaxel to 8.81~9.58 nM, for Doxorubicin to 102~1260 nM[1].

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

P-gp inhibitor 5 相关抗体:
分子量

517.98

Formula

C28H20ClNO5S
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

P-gp inhibitor 5 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 52451298-06-7P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243KBvinVincristinePaclitaxelDoxorubicinmultidrug resistanceantiproliferativeInhibitorinhibitorinhibit

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目录号：
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