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 (356)
Antibodies (3)

By Effects:	Inhibitors (259)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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.

HY-176287

ARN25657	Inhibitor
ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC₅₀ = 15.2 nM, K_i=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.

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.

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.

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.

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.

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.

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.

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.

HY-W787758

2-Propylpent-4-ynoic acid	Inhibitor
2-Propylpent-4-ynoic acid (4-yn-VPA) is a HDAC inhibitor (with an IC₅₀ of 0.5 mM against human HDAC). 2-Propylpent-4-ynoic acid also induces P-glycoprotein function, and exhibits teratogenicity, fetal growth inhibition and neurotoxicity. 2-Propylpent-4-ynoic acid shows significant stereospecific teratogenic effects, with the S-enantiomer being more teratogenic than the R-enantiomer and other analogs. The neurotoxicity of 2-Propylpent-4-ynoic acid is independent of its stereochemical structure. 2-Propylpent-4-ynoic acid has been used in studies related to the pathogenesis of colon cancer and neural tube defects such as exencephaly.

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.

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.

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.

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.

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.

HY-D1005A9

Poloxamer 183 (L63)	Inhibitor
Poloxamer 183 L63 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 2000. Poloxamer has the ability to inhibit P-gp. Poloxamer 183 exhibits antimicrobial activity and can inhibit Mycobacterium avium. Poloxamer 183 can be used as a cosmetic ingredient.

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.

HY-W754548

Glycocholic acid-¹³C₂,d₄N	Inhibitor
Glycocholic acid-¹³C₂,d₄ is the deuterium labeled and ¹³C-labeled Glycocholic acid (HY-N1423). Glycocholic acid 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 inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

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>.

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P-glycoprotein

P-glycoprotein

P-glycoprotein Related Products (356)

Antibodies (3)

P-glycoprotein Related Products (356):