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197226 Sigma-Aldrich

BCRP Inhbitor - Calbiochem

The BCRP Inhbitor controls the biological activity of BCRP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym: BCRP Inhbitor - Calbiochem, N-(4-(2-hydroxyethyl)phenyl)-2-(4-nitrobenzamido)benzamide

  • Empirical Formula (Hill Notation) C22H19N3O5

  • Molecular Weight 405.40

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Properties

Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   off-white
solubility   DMSO: 100 mg/mL
shipped in   ambient

Description

General description

A non-tetrahydroisoquinoline BCRP specific inhibitor based on the anthranilic acid scaffold, that displays an IC50 of 1.39 µM in a Hoechst 33343 assay in stably transfected MDCK BCRP cells, which is ˜50-fold more potent than novobiocin (IC50 = 65 µM), and shows no effect towards other ATP binding cassette (ABC) transporters P-gp and MRP1 at up to a concentration of 10 µM. It is shown to be an allosteric inhibitor in enzyme kinetics assays in the presence of BCRP specific substrates pheophorbide A and imitanib, and does not lead to a decrease in cell viability up to a concentration of 10 µM.

Packaging

10 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Pick, A. et al. 2010. Chem. Med. Chem.5, 1498.
Klinkhammer, W., et al. 2009. Bioorg. Med. Chem.17, 2524.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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