1. Membrane Transporter/Ion Channel
  2. BCRP
  3. ABCG2-IN-3

ABCG2-IN-3 (Compound 52) 是乳腺癌耐药蛋白 (ABCG2) 的选择性抑制剂,IC50 为 0.238 µM 。ABCG2-IN-3 克服 ABCG2 介导的对 SN-38 的抗性并抑制 ATPase 活性。

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ABCG2-IN-3 Chemical Structure

ABCG2-IN-3 Chemical Structure

CAS No. : 1942919-63-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDCK-II GI50
4.67 μM
Compound: 51
Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 27280693]
MDCK-II GI50
4.83 μM
Compound: 51
Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 27280693]
Sf9 IC50
0.026 μM
Compound: 51
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method
[PMID: 27280693]
Sf9 IC50
0.285 μM
Compound: 51
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method
[PMID: 27280693]
体外研究
(In Vitro)

ABCG2-IN-3 对细胞 MDCK II BCRP 和 MDCK 野生型具有细胞毒性,CI50s 分别为 5.82 和 6.55 μM[1]
ABCG2-IN-3 抑制 ATPase,IC50 为 0.038 μM[1]

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

分子量

451.34

Formula

C25H20Cl2N2O2

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
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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.

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产品名称:
ABCG2-IN-3
目录号:
HY-119724
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