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-14794A
    Levomilnacipran
    		Substrate
    Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
    Levomilnacipran
  • 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-130133
    DHW-221
    		Inhibitor
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
    DHW-221
  • 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-173182
    Antitumor agent-200
    Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field.
    Antitumor agent-200
  • 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-176287
    ARN25657
    		Inhibitor
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.
    ARN25657
  • 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-180282
    P-gp-IN-33
    		Inhibitor
    P-gp-IN-33 (Compound 17a) is a P-gp inhibitor. P-gp-IN-33 binds the Verapamil (HY-14275)-binding pocket of P-gp. P-gp-IN-33 shows higher cytotoxicity against resistant non-small cell lung carcinoma cells than against non-resistant non-small cell lung carcinoma cells.
    P-gp-IN-33
  • HY-181773
    P-gp-IN-36
    		Inhibitor
    P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. P-gp-IN-36 inhibits the efflux function of P-glycoprotein, overcoming P-gp-mediated multidrug resistance in cancer cells. P-gp-IN-36 inhibits STAT3 phosphorylation and reduces total STAT3 expression. P-gp-IN-36 sensitizes P-gp-expressing cancer cells to the cytostatic effects of conventional cytostatic drugs. P-gp-IN-36 can be used for the research of multidrug-resistant cancer.
    P-gp-IN-36
  • 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-182253
    WS-691
    		Modulator
    WS-691 is an orally active, selective ABCB1 modulator. WS-691 selectively stabilizes ABCB1 via direct binding to ABCB1. WS-691 inhibits the efflux function of ABCB1 and activates ABCB1 ATPase activity. WS-691 elevates intracellular Paclitaxel (HY-B0015) levels and reduces the required dose of Paclitaxel in cancer cells overexpressing ABCB1. WS-691 increases the sensitivity of colon cancer cells to Paclitaxel.
    WS-691
  • 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
  • HY-14794AS
    Levomilnacipran-d10 hydrochloride
    		Substrate
    Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
    Levomilnacipran-d<sub>10</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity