2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. P-glycoprotein

P-glycoprotein

P-gp; Pgp; Multidrug resistance protein 1; MDR1; ATP-binding cassette sub-family B member 1; ABCB1; Cluster of differentiation 243; CD243

P-glycoprotein

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P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-159085
    P-gp inhibitor 24
    		Inhibitor
    P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrug resistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells.
    P-gp inhibitor 24
  • HY-B0532AS
    Trifluoperazine-d3 dihydrochloride
    		Inhibitor
    Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
    Trifluoperazine-d<sub>3</sub> dihydrochloride
  • HY-N0633R
    Muscone (Standard)
    Muscone (Standard) is the analytical standard of Muscone. This product is intended for research and analytical applications. Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.
    Muscone (Standard)
  • HY-106035
    Tyroservatide
    		Inhibitor
    Tyroservatide (YSV) is an active, low-molecular-weight polypeptide that has been shown to have antitumor effects on hepatocellular carcinoma and lung cancer cell.
    Tyroservatide
  • HY-163204
    RhQ-DMB
    		Inhibitor
    RhQ-DMB is a potent inhibitor of P-gp. RhQ-DMB exhibits high affinity and inhibitory activity in yeast strains expressing CmABCB1.
    RhQ-DMB
  • HY-168008
    P-gp inhibitor 25
    		Inhibitor
    P-gp inhibitor 25 (compound 16c) is a P-gp inhibitor. P-gp inhibitor 25 can enhance the oral absorption of paclitaxel (HY-B0015). P-gp inhibitor 25 can be used in anti-cancer research.
    P-gp inhibitor 25
  • HY-135328S
    Norverapamil-d7
    		Inhibitor
    Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
    Norverapamil-d<sub>7</sub>
  • HY-N0450R
    Sinapine (thiocyanate) (Standard)
    		Inhibitor
    Sinapine (thiocyanate) (Standard) is the analytical standard of Sinapine (thiocyanate). This product is intended for research and analytical applications. Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
    Sinapine (thiocyanate) (Standard)
  • HY-126906R
    Milbemycin A4 (Standard)
    		Inhibitor
    Milbemycin A4 (Standard) is the analytical standard of Milbemycin A4. This product is intended for research and analytical applications. Milbemycin A4 inhibits P-glycoprotein activity, and reverses multidrug resistance of tumor cells. Milbemycins are a family of macrolide antibiotics with insecticidal and acaricidal activitysup>.
    Milbemycin A4 (Standard)
  • HY-N6684R
    Deoxynivalenol (Standard)
    Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors.
    Deoxynivalenol (Standard)
  • HY-N11424
    Bilirubin diglucuronide
    		Inhibitor
    Bilirubin diglucuronide is the metabolite of Bilirubin (HY-N0323). Bilirubin diglucuronide inhibits MRP1/2 mediated ATP-dependent transport of leukotriene C4 (LTC4) in membrane vesicles.
    Bilirubin diglucuronide
  • HY-15206R
    Glibenclamide (Standard)
    		Inhibitor
    Glibenclamide (Standard) is the analytical standard of Glibenclamide. This product is intended for research and analytical applications. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
    Glibenclamide (Standard)
  • HY-N1514R
    Ganoderenic acid B (Standard)
    Doxylamine (succinate) (Standard) is the analytical standard of Doxylamine (succinate). This product is intended for research and analytical applications. Doxylamine (succinate), a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent.
    Ganoderenic acid B (Standard)
  • HY-120931
    LY329146
    		Inhibitor
    LY329146, a Raloxifene (HY-13738) analog, is multidrug resistance protein (MRP1) inhibitor. LY329146 inhibits leucotriene C4 ( LTC4) transport with an IC50 of 0.8 μM.
    LY329146
  • HY-163918
    N,N-Dimethyl-idarubicin
    N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells.
    N,N-Dimethyl-idarubicin
  • HY-136934
    Reversin 205
    		Inhibitor
    Reversin 205 ([Boc-Glu(Obzl)]2-Lys-Ome) is a P-glycoprotein (ABCB1) inhibitor. Reversin 205 is a peptide chemosensitizer.
    Reversin 205
  • HY-N3584R
    Paris saponin VII (Standard)
    		Inhibitor
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII (Standard)
  • HY-N10491
    Spongionellol A
    		Inhibitor
    Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer.
    Spongionellol A
  • HY-17367S4
    Atazanavir-d6
    		Modulator 99.28%
    Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
    Atazanavir-d<sub>6</sub>
  • HY-150565
    P-gp inhibitor 5
    		Inhibitor
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
    P-gp inhibitor 5
Cat. No. Product Name / Synonyms Application Reactivity