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-135336BS
    (Rac)-Verapamil-d7 hydrochloride
    (Rac)-Verapamil-d7 (hydrochloride) is the deuterium labeled (Rac)-Verapamil[1].
    (Rac)-Verapamil-d<sub>7</sub> hydrochloride
  • HY-168711
    P-gp inhibitor 27
    		Inhibitor
    P-gp inhibitor 27 (Compound D2) is an inhibitor for P-glycoprotein (P-gp), that downregulates the expression of P-gp and MRP1, increases the Rh123 accumulation in A2780/T cell, and reverses multidrug resistance to Paclitaxel (HY-B0015) (EC50 is 88 nM) and Cisplatin (HY-17394).
    P-gp inhibitor 27
  • HY-P10856
    CPI1
    		Inhibitor
    CPI1 is a potent and highly specific multidrug resistance protein 1 (MRP1) inhibitor. CPI1 inhibits MRP1 (Ki: 100 nM) with nanomolar potency but shows minimal inhibition of P-glycoprotein (Pgp). CPI1 and LTC4 compete to bind to the same site of MRP1, inhibiting ATP hydrolysis and substrate transport. CPI1 can be used to study drug delivery and chemotherapy resistance in cancer.
    CPI1
  • HY-121088
    Ceefourin 2
    		Inhibitor
    Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability.
    Ceefourin 2
  • HY-162714
    C3N-Dbn-Trp2
    		Inhibitor
    C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells.
    C3N-Dbn-Trp2
  • HY-11018S2
    Risperidone-d6
    		Inhibitor
    Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
    Risperidone-d<sub>6</sub>
  • HY-15134
    ONT-093
    		99.21%
    ONT-093 is a potent inhibitor of P-glycoprotein pump. ONT-093 has the potential for the research cancer diseases.
    ONT-093
  • HY-162040
    P-gp inhibitor 17
    		Inhibitor
    P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study.
    P-gp inhibitor 17
  • HY-161776
    P-gp/CDK2-IN-1
    		Inhibitor
    P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment.
    P-gp/CDK2-IN-1
  • HY-149981
    P-gp inhibitor 13
    		Inhibitor
    P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia.
    P-gp inhibitor 13
  • HY-158435
    P-gp inhibitor 23
    		Inhibitor
    P-gp inhibitor 23 (compound 14F) is a potent inhibitor of P-gp and CYP3A4, with the EC50 and IC50 of 28 nM and 223 nM, respectively.
    P-gp inhibitor 23
  • HY-149053B
    (R)-OY-101
    		Inhibitor
    (R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research.
    (R)-OY-101
  • HY-116976
    NSC-57969
    NSC-57969 is a multidrug resistant (MDR)-selective agent, exhibiting a robust Pgp-dependent toxic activity across diverse cancer cell lines.
    NSC-57969
  • HY-N1514
    Ganoderenic acid B
    		99.61%
    Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
    Ganoderenic acid B
  • HY-N0069R
    Solamargine (Standard)
    		Inhibitor
    Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
    Solamargine (Standard)
  • HY-B0947S1
    Sulfanitran-13C6
    		Activator
    Sulfanitran-13C6 is the 13C labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
    Sulfanitran-<sup>13</sup>C<sub>6</sub>
  • HY-149240
    Anticancer agent 108
    		Inhibitor
    Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice.
    Anticancer agent 108
  • HY-162369
    PID-9
    		Inhibitor
    PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrug resistance (MDR) reversal activity (IC50 = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression.
    PID-9
  • HY-N3197
    Neostenine
    		Inhibitor
    Neostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application.
    Neostenine
  • HY-13574
    Biricodar dicitrate
    		Inhibitor
    Biricodar dicitrate (VX 710-3) is the dicitrate salt form of Biricodar (HY-13574A). Biricodar dicitrate is an inhibitor for P-glycoprotein and multidrug resistance-associated protein 1 (MRP-1), which increases the accumulation of chemotherapy drugs within cancer cells and shows effective chemosensitizing activity in multidrug resistant cells.
    Biricodar dicitrate
Cat. No. Product Name / Synonyms Application Reactivity