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Ko134 - BCRP Specific Inhibitor

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SB Ko134 250 μg/1 mg/ 5mg BCRP

Description

SOLVO Biotechnology offers Ko134 for ABCG2/BCRP membrane transporter inhibition studies.

Ko134, the tetracyclic fumitremorgin C (FTC) analog, is a highly potent and specific inhibitor of the ABCG2 (BCRP) multidrug transporter protein.
Our data show that Ko-134 inhibits BCRP with IC50 0.070 µM and it inhibits P-gp at IC50 > 1 µM. Contrarily, GF120918 - a model P-gp inhibitor - more potently inhibits P-gp (IC50=0.132) than BCRP (IC50=7.906). Additional data were published by Allen et al, 2002 (1).

 P-gp IC50
(µM)		BCRP IC50
(µM)
Ko134>10.070
GF1209180.1327.906

Due to its non-toxic property at its effective concentrations both in vivo and in vitro, Ko134 is an excellent laboratory reagent.


Figure 1. Inhibitory effect of Ko134 on Hoechst 33342 (BCRP substrate) efflux in a fluorescent whole cell based assay.


Figure 2. Inhibition of the vanadate sensitive ATPase activity of SB-BCRP-Sf9 preparations by Ko134


Figure 3. Inhibition of the vanadate sensitive ATPase activity of SB-BCRP-M preparations by Ko134


Figure 4. Ko134 enhanced SN-38 (BCRP substrate anticancer agent) cytotoxicity in BCRP expressing P388 cells at various concentrations

References
1. John D. Allen, Arnold van Loevezijn, Jeany M. Lakhai, Martin van der Valk,Olaf van Tellingen, Glen Reid, Jan H. M. Schellens,Gerrit-Jan Koomen, and Alfred H. Schinkel (2002) Molecular Cancer Therapeutics Vol. 1, 417-425
2. Glavinas H., et al., ABCG2 (breast cancer resistance protein/mitoxantrone resistance-associated protein) ATPase assay: a useful tool to detect drug-transporter interactions. Drug Metab Dispos. 35(9):1533-42, (2007)
3. Pál A., et al., Cholesterol potentiates ABCG2 activity in a heterologous expression system: improved in vitro model to study function of human ABCG2. J. Pharmaco.l Exp. Ther. 321(3):1085-94, (2007).
4. Van Loevezijn, A., et al., Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg. Med. Chem. Lett. 11, 29-32, (2001)

Reference:

  1. Constitutive mRNA expression and protein activity levels of nine ABC efflux transporters in seven permanent cell lines derived from different tissues of rainbow trout
    Stephan Fischer, Jovica Loncar, Roko Zaja, Sabine Schnel, Kristin Schirmer, Tvrtko Smital and Till Luckenbach