P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein -mediated multidrug resistance. In Vitro P-gp inhibitor 1 (12k) possesses high potency ( EC 50 =57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes). P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: K562/A02 cell Concentration: 0.1, 0.5, or 2.0 μM Incubation Time: 72 hours Result: MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux. Form:Solid IC50& Target:P-glycoprotein
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P-gp inhibitor 1
CAS number:2050747-49-2 molecular formula:C32H31N5O2
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| Chinese alias | P-gp 抑制剂 1 | ||
| English alias | - | ||
| CAS number | 2050747-49-2 | molecular formula | C32H31N5O2 |
| molecular weight | 517.62 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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