2. Membrane Transporter/Ion Channel
  3. BCRP
  4. Pentamethoxymorin

Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC50 vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer.

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Pentamethoxymorin

Pentamethoxymorin Chemical Structure

CAS No. : 7555-80-8

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Pentamethoxymorin Related Antibodies

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Description

Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC50 vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer[1].

Cellular Effect
Cell Line Type Value Description References
A2780 ADR IC50
27.1 μM
Compound: 11
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
[PMID: 23851114]
MDCK-II IC50
5.94 μM
Compound: 11
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
[PMID: 23851114]
MDCK-II IC50
5.98 μM
Compound: 11
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
[PMID: 23851114]
In Vitro

Pentamethoxymorin (compound 11) (0.031-100 µM; 30 min-72 h) inhibits BCRP and weakly inhibits P-gp, with no MRP1 inhibition and low cytotoxicity (IC50 = 5.94-5.98 μM for BCRP, 27.1 μM for P-gp)[1].

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

Pentamethoxymorin Related Antibodies
Molecular Weight

372.37

Formula

C20H20O7
CAS No.
SMILES

O=C1C(OC)=C(OC2=CC(OC)=CC(OC)=C21)C=3C=CC(OC)=CC3OC
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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Pentamethoxymorin Related Classifications

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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.

Keywords:

Pentamethoxymorin7555-80-8MRS923MRS 923MRS-923BCRPBreast cancer resistance proteinABCG2P-gp-overexpressing cellsBCRP/ABCG2P-gpMRP1Breast Cancer Resistance ProteinBCRP substratesP-glycoproteinBCRP-expressing cellsMultidrug resistance-associated protein 1MRP1-overexpressing cellsInhibitorinhibitorinhibit

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