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P-glycoprotein (P-gp) inhibitors block a drug efflux pump that contributes to multidrug resistance in cells. P-gp, also called multidrug resistance protein 1 (MDR1) or ATP-binding cassette subfamily B member 1 (ABCB1), uses energy from adenosine triphosphate (ATP) hydrolysis. It was first described in 1976 as a surface glycoprotein of drug-resistant Chinese hamster ovary cells. A crystal structure later showed a large drug-binding pocket that accounts for its broad substrate range. Verapamil and its metabolite norverapamil hydrochloride are early inhibitors, and verapamil is also listed under Calcium Channels. Later inhibitors include valspodar, tariquidar, LY335979 and elacridar, which also blocks breast cancer resistance protein (BCRP).
Synonyms: (±)-Norverapamil hydrochloride; D591 hydrochloride
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
Synonyms: CP-16533-1; ±-Verapamil
Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
Synonyms: RTA 744; WP 744; WP 769 hydrochloride
Berubicin hydrochloride is an NF-kB agonist and a Doxorubicin analog with the ability to cross the blood-brain barrier. It inhibits P-glycoprotein (P-gp) and multidrug resistance-associated protein 1 (MRP1), thereby reducing efflux in glioblastoma multiforme (GBM) and exerting cytotoxic effects on leukemia cells. Additionally, Berubicin hydrochloride induces apoptosis in neuroblastoma cells, making it a valuable reagent for studying tumors of the nervous system.
Roquefortine C is a mycotoxin derived from Penicillium species, exhibiting multiple biological activities. As an agonist of P-glycoprotein (P-gp), it inhibits cytochrome P450 enzymes, specifically P450 3A and P450 1A. This compound demonstrates antimicrobial effects against Gram-positive bacteria and possesses neurotoxic properties, along with potential antitumor activity. Roquefortine C serves as a valuable tool in research exploring microbial interactions and pharmacological mechanisms.
Synonyms: (±)-Norverapamil; D591
Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations.
MCI826 is a P-glycoprotein (P-gp) agonist that enhances the efflux of various substrates across cell membranes. Its primary biological activity focuses on modulating drug transport and influencing cellular drug accumulation. This compound is valuable in research applications related to pharmacokinetics, multidrug resistance, and therapeutic strategies involving P-gp.
