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.

P-glycoprotein Related Products (355)
Antibodies (3)

By Effects:	Inhibitors (259)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-173162

GPV0057	Inhibitor	99.20%
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel K_ir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of K_ir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, K_ir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.

HY-125486

Reversin 121	Inhibitor	99.08%
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers.

HY-A0064R

Verapamil hydrochloride (Standard)	Inhibitor
Verapamil (hydrochloride) (Standard) is the analytical standard of Verapamil (hydrochloride). This product is intended for research and analytical applications. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.

HY-N1457

Chrysosplenetin	Inhibitor	99.84%
Chrysosplenetin is an orally active polymethoxyflavone. Chrysosplenetin exerts anticancer effects by inhibiting topoisomerase, protecting DNA and inducing apoptosis. Chrysosplenetin acts as an antimalarial sensitizer, reverses Artemisinin (HY-B0094) resistance by inhibiting and downregulating P-glycoprotein, and enhances the efficacy of Artemisinin. Chrysosplenetin promotes bone formation by activating the Wnt/β-catenin pathway and exerts anti-osteoporotic effects.

HY-P990196

Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)	Inhibitor
Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer.

HY-D1005A23

Poloxamer 401 (L121)	Inhibitor
Poloxamer 401 L121 is a block copolymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 4400. Poloxamer has the ability to inhibit P-gp. Poloxamer 401 inhibits multiagent resistance and adjuvant activity. Poloxamer 401 can be used as a cosmetic ingredient. Poloxamer 401 can be used in nanoparticle engineering (lymphatic targeting particles) research.

HY-N6015

Bacopasaponin C	Inhibitor	99.76%
Bacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated P-gp ATPase activity with an IC₅₀ of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani.

HY-132189

Laniquidar	Inhibitor	99.42%
Laniquidar is a non-competitive P-gp inhibitor with an IC₅₀ of 0.51 μM. Laniquidar binds to the P-gp transporter with high affinity and exhibits low activity as a substrate. Laniquidar is applicable to epilepsy-related research.

HY-N6932

Voacamine	Inhibitor	99.64%
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer.

HY-D1005A8

Poloxamer 181 (L61)	Inhibitor
Poloxamer 181 L61 is a block polymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 2000. Poloxamer has the ability to inhibit P-gp. Poloxamer 181 has antimicrobial activity and can inhibit Mycobacterium avium. Poloxamer 181 can form a thermally reversible hydrogel and is used as a food additive, and as an agent delivery carrier in cosmetics, pharmaceuticals and tissue engineering.

HY-N0144R

Piperine (Standard)	Inhibitor
Piperine (Standard) is the analytical standard of Piperine. This product is intended for research and analytical applications. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL.

HY-N2947

Boeravinone B	Inhibitor
Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress.

HY-119823

PGP-4008	Inhibitor	99.26%
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin.

HY-N1423B

Glycocholic acid hydrate	Inhibitor
Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

HY-113805

MC70	Inhibitor	99.50%
MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC₅₀ of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1.

HY-126906

Milbemycin A4	Inhibitor	99.13%
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>[2].

HY-N7641

3',4',7-Trimethoxyquercetin	Inhibitor	98.87%
3',4',7-Trimethoxyquercetin (Quercetin 3′,4′,7-trimethyl ether) is a polymethoxyflavonoid that can be isolated from Taraxacum mongolicum. 3',4',7-Trimethoxyquercetin is also a derivative of Quercetin hydrate (HY-18085A). 3',4',7-Trimethoxyquercetin has anti-tumor activity.

HY-15206S

Glyburide-d₁₁	Inhibitor	99.39%
Glyburide-d₁₁ is the deuterium labeled Glibenclamide. 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.

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.

HY-123742

Estradiol 3-sulfate 17-glucuronide potassium	Inhibitor	99.92%
Estradiol 3-sulfate 17-glucuronide potassium is metabolite of estradiol. Estradiol 3-sulfate 17-glucuronide potassium inhibits multidrug resistance protein (MRP) mediated 17β -Estradiol 17-(β -D-Glucuronide) transport with a K_i of 22 μM.

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P-glycoprotein

P-glycoprotein

P-glycoprotein Related Products (355)

Antibodies (3)

P-glycoprotein Related Products (355):