A cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01-1uM) without altering the BCRP expression levels (in <6hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC50>10uM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available.
Formula:C₂₀H₂₂N₂O₃S
Molecular Weight:370.5
Solubility:DMSO (100mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
