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

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.

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ABCG2-IN-3 Chemical Structure

ABCG2-IN-3 Chemical Structure

CAS No. : 1942919-63-2

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Description

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].

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]
In Vitro

ABCG2-IN-3 exhibits a cytotoxicity against cells MDCK II BCRP and MDCK wild-type, with CI50s of 5.82 and 6.55 μM[1].
ABCG2-IN-3 inhibits ATPase with an IC50 of 0.038 μM[1].

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

Molecular Weight

451.34

Formula

C25H20Cl2N2O2

CAS No.
SMILES

COC1=CC=C(C=C1)C(N2C(C3=C(CC2)C(C=CC=C4)=C4N3)C5=CC(Cl)=C(C=C5)Cl)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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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Product Name:
ABCG2-IN-3
Cat. No.:
HY-119724
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