|LY335979 (Zosuquidar 3HCL)Pgp (P-glycoprotein) inhibitor|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Description||Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with a Ki value of 60 nM.|
|Cas No.||167465-36-3||SDF||Download SDF|
|Synonyms||RS 33295-198; Zosuquidar trihydrochloride; LY335979; LY-335979|
|Chemical Name||(R)-1-(4-((1aR,6s,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
LY335979 is a selective inhibitor of P-Gp with IC50 value of 1.2 nM [1, 2].
P-gp (P-glycoprotein) is a member of ATP-binding cassette (ABC) transporters and plays a pivotal role in pumping many foreign substances out of cells. It has been reported that abnormal expression of P-Gp is correlated with the multidrug resistance of tumor cells .
LY335979 is a potent P-Gp inhibitor and has a different selectivity with the reported P-Gp inhibitor cyclosporin A or verapamil. In drug-resistant cell line HL60/VCR with highly expression of P-Gp, LY335979 exhibited highly restore ability of P-Gp than cyclosporin A or verapamil and the IC 50 value of 1.2 nM . When tested with a panel of cell lines over-expressed P-Gp (CEM/VLB100, MCF-7/ADR, 2780AD, P388/ADR, and UCLA-P3.003VLB), administration of LY335979 reversed the cells resistance to Vinblastine, Doxorubicin, Btoposide and Taxol by inhibiting P-Gp activity .
In female nude mice model with UCLA-P3.003VLB MDR tumor cells subcutaneous xenograft, pre-treated with LY335979 (30mg/kg) restored tumor cells sensitivity to Taxol (20 mg/kg) which combination markedly suppressed solid tumor growth compared with control group .
1. Green, L.J., P. Marder, and C.A. Slapak, Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. Biochem Pharmacol, 2001. 61(11): p. 1393-9.
2. Dantzig, A.H., et al., Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res, 1996. 56(18): p. 4171-9.
3. Hu, T., et al., Reversal of P-glycoprotein (P-gp) mediated multidrug resistance in colon cancer cells by cryptotanshinone and dihydrotanshinone of Salvia miltiorrhiza. Phytomedicine, 2014. 21(11): p. 1264-72.