MCI826

Names

[ Name ]:
MCI826

[Synonym ]:
2,2-Diethyl-4-({3-[(E)-2-(4-isopropyl-1,3-thiazol-2-yl)vinyl]phenyl}amino)-4-oxobutanoic acid
Butanoic acid, 2,2-diethyl-4-[[3-[(E)-2-[4-(1-methylethyl)-2-thiazolyl]ethenyl]phenyl]amino]-4-oxo-

Biological Activity

[Description]:

MCI826 is a P-glycoprotein (P-gp) antagonist.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

Research Areas >> Cancer

[Target]

P-glycoprotein[1]

[In Vitro]

Verapamil and cyclosporine A, first-generation modulators, and MCI826 (VX-710), a third generation P-gp modulator, are effective enhancers of C6-ceramide response in cells. Verapamil and MCI826 demonstrate weak cytotoxicity alone; however, when administered with C6-ceramide, which is only moderately cytotoxic, viability fell precipitously[1].

[Cell Assay]

Cells are seeded in 96-well plates. Drugs (including MCI826 (VX-710)) are diluted freshly into culture medium containing 1% FBS and added to wells to a total volume of 0.2 mL, thus the final concentration of FBS during treatment is 5.5%. After addition of agents, cells are incubated at 37°C for 72 or 96 hr, and cell viability is determined using cell proliferation assay kit[1].

[References]

[1]. Morad SA, et al. Tamoxifen magnifies therapeutic impact of ceramide in human colorectal cancer cells independent of p53. Biochem Pharmacol. 2013 Apr 15;85(8):1057-65.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C₂₂H₂₈N₂O₃S

[ Molecular Weight ]:
400.534

[ Exact Mass ]:
400.182068

[ LogP ]:
4.87

[ Index of Refraction ]:
1.628

[ Storage condition ]:
2-8℃

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.