P-gp

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).

3 Items

  • Berubicin hydrochloride
    Cat. No.
    A25165

    Berubicin hydrochloride

    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.

    1 mg
    $195.00
    5 mg
    $510.00
    All 2 sizes
  • Roquefortine C
    Cat. No.
    A34309

    Roquefortine C

    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.

    0.5 mg
    $135.00
    1 mg
    $240.00
    All 2 sizes
  • MCI826
    Cat. No.
    A67878

    MCI826

    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.

    1 mg
    $560.00
    5 mg
    $1,475.00
    All 2 sizes

3 Items

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