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-178466
    Tubulin polymerization/P-gp-IN-1
    		Inhibitor
    Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer.
    Tubulin polymerization/P-gp-IN-1
  • HY-W230975
    (E/Z)-Piperine
    		Inhibitor 98.91%
    (E/Z)-Piperine ((E/Z)-Bioperine) is an alkaloid with a pungent property. (E/Z)-Piperine shows anti-inflammation, immunomodulatory and anti-cancer, antispasmodic and anti-secretory effects. (E/Z)-Piperine demonstrates significant neuroprotective effect in Alzheimer’s disease and Parkinson’s disease.
    (E/Z)-Piperine
  • HY-121247
    Bromotetrandrine
    		Inhibitor
    Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment.
    Bromotetrandrine
  • HY-W702907
    DM-4103
    		Inhibitor
    DM-4103 is a major metabolite of Tolvaptan (HY-17000) that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4103 inhibits the ability of human liver transporters NTCP, BSEP, MRP2, MRP3, MRP4 (IC50 values are 16.3, 4.15, 51.0, 44.6, 4.26 μM, respectively) and bile acid transport in SCHH cells. DM-4103 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD).
    DM-4103
  • HY-100750R
    Norverapamil hydrochloride (Standard)
    		Inhibitor
    Norverapamil (hydrochloride) (Standard) is the analytical standard of Norverapamil (hydrochloride). This product is intended for research and analytical applications. 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[1][2].
    Norverapamil hydrochloride (Standard)
  • HY-107212R
    Selamectin (Standard)
    		Inhibitor
    Selamectin (Standard) is the analytical standard of Selamectin. This product is intended for research and analytical applications. Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
    Selamectin (Standard)
  • HY-N1423AR
    Glycocholic acid sodium (Standard)
    		Inhibitor
    Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid sodium (Standard)
  • HY-W702292
    (R)-(+)-Verapamil-d6 hydrochloride
    		Inhibitor
    (R)-(+)-Verapamil-d6 (hydrochloride) is deuterium labeled (R)-Verapamil (hydrochloride). (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents.
    (R)-(+)-Verapamil-d<sub>6</sub> hydrochloride
  • HY-161353
    c-Met-IN-23
    		Inhibitor
    c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC50 = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent.
    c-Met-IN-23
  • HY-181804
    MRS8288
    		Inhibitor
    MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC50 of 0.96 μM against ABCG2 and an IC50 of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research.
    MRS8288
  • HY-129841
    Niguldipine monohydrochloride
    		Inhibitor
    Niguldipine monohydrochloride is a calcium channel blocker that inhibits P-glycoprotein and can be used in tumor research. Niguldipine monohydrochloride inhibits Cav 3.2, with an IC50 of 0.9 μM.
    Niguldipine monohydrochloride
  • HY-178382
    BRAFV600E/ABL2-IN-1
    		Inhibitor
    BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.
    BRAFV600E/ABL2-IN-1
  • HY-175522
    P-gp-IN-31
    		Inhibitor
    P-gp-IN-31 is a P-glycoprotein (P-gp) inhibitor with IC50 values of 0.42 μM for KB cells and 0.43 μM for MDR KBvin cells. P-gp-IN-31 can pass P-gp-mediated drug efflux mechanisms and shows collateral sensitivity via P-gp downregulation. P-gp-IN-31 inhibits cell proliferation, induces apoptosis and arrests the cell cycle at G2/M phase. P-gp-IN-31 can be used for the research of cancer, such as multidrug-resistant (MDR) malignancies.
    P-gp-IN-31
  • HY-179683
    MRP1-IN-2
    		Inhibitor
    MRP1-IN-2 (Compound 21) is a selective MRP1 inhibitor with a relatively weak inhibitory effect on P-gp. MRP1-IN-2 exhibits a strong accumulation effect of calcein, with its EC50 value being 177 nM. MRP1-IN-2 enhances the activity of Doxorubicin (HY-15142A) on drug-resistant cells. MRP1-IN-2 can be used for the study of multidrug-resistant cancers.
    MRP1-IN-2
  • HY-162822
    P-gp modulator-5
    		Modulator
    P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles.
    P-gp modulator-5
  • HY-N17304
    10S,13aR-Antofine N-oxide
    		Substrate
    10S,13aR-Antofine N-oxide is a phenanthroindolizidine N-oxide alkaloid and cytotoxic agent found in Cynanchum vincetoxicum. 10S,13aR-Antofine N-oxide exerts cytotoxic effects in drug-sensitive (KB-3-1, IC50 = 0.11 μM) and multi-drug-resistant (KB-V1, IC50 = 0.16 μM) carcinoma cells. 10S, 13aR-Antofine N-oxide acts as a poor substrate for the P-glycoprotein (P-170) efflux pump. 10S,13aR-Antofine N-oxide can be used for the research of cancers.
    10S,13aR-Antofine N-oxide
  • HY-123793
    MK-1832
    MK-1832 (Compound 32) is a selective Kv1.5 inhibitor (IC50 = 86 nM). MK-1832 is a P-glycoprotein substrate. MK-1832 can be used in atrial fibrillation research.
    MK-1832
  • HY-178349
    P-gp inhibitor 30
    		Inhibitor
    P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis, induces autophagy, and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research.
    P-gp inhibitor 30
  • HY-146389
    Anticancer agent 50
    		Modulator
    Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
    Anticancer agent 50
  • HY-174469
    PROTAC PI3K/110β degrader-2
    		Inhibitor
    PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)).
    PROTAC PI3K/110β degrader-2
Cat. No. Product Name / Synonyms Application Reactivity