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Results for "

multidrug efflux

" in MedChemExpress (MCE) Product Catalog:

By Targets:	P-glycoprotein (26) Adrenergic Receptor (1) Antibiotic (1) Apoptosis (3) Bacterial (10) BCRP (2) Calcium Channel (2) DNA-PK (1) Drug Derivative (1) Endogenous Metabolite (2) Farnesyl Transferase (1) FOXO (2) Histamine Receptor (2) MDM-2/p53 (2) NF-κB (4) Parasite (4) PI3K (1) Potassium Channel (1) Protein Arginine Deiminase (2) Reactive Oxygen Species (ROS) (2) Reference Standards (3)
By Research Areas:	Cancer (30) Cardiovascular Disease (1) Infection (8) Inflammation/Immunology (5) Metabolic Disease (2) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Targets Recommended: P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156753

NorA-IN-1	Bacterial	Cancer
NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance .

HY-15134

ONT-093 OC 144-093; OC 144093	P-glycoprotein	Infection Cancer
ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC₅₀ of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial .

HY-N3308

Medicarpin 2 Publications Verification	Apoptosis	Cancer
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of agents .

HY-P10874

SMR efflux inhibitor	Bacterial	Infection
SMR efflux inhibitor targets the small multidrug resistance (SMR) efflux pump, blocks the interaction of TM4-TM4, and exhibits board-spectrum antibacterial activity .

HY-N11697

α-Cryptoxanthin	P-glycoprotein	Cancer
α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump .

HY-117763

A-39355	Calcium Channel	Others
A-39355 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-39355 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.

HY-120768

A-30312	Drug Derivative	Others
A-30312 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-30312 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.

HY-13766A

Timcodar mesylate VX-853-2	Bacterial	Others
Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .

HY-129279

Andrastin A	Farnesyl Transferase	Cancer
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .

HY-120790

S 16317	Calcium Channel P-glycoprotein	Cancer
S 16317 is an orally active dihydropyridine derivative with low calcium channel affinity (K_i: 0.55 μM). S 16317 inhibits P-gp mediated efflux of ADR. S 16317 overcomes multidrug resistance in tumor .

HY-146117

P-gp modulator 2	P-glycoprotein	Cancer
P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .

HY-146118

P-gp modulator 3	P-glycoprotein	Cancer
P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .

HY-N15297

Isotenulin	P-glycoprotein	Cancer
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .

HY-N0406

2"-O-beta-L-galactopyranosylorientin	P-glycoprotein	Inflammation/Immunology
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2). Anti-inflammatory effect .

HY-162822

P-gp modulator-5	P-glycoprotein	Cancer
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 .

HY-17013A

Dofequidar fumarate 2 Publications Verification MS-209	P-glycoprotein	Cancer
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-161645

P-gp modulator-4	P-glycoprotein	Cancer
P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC₅₀ of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8) .

HY-144366

P-gp inhibitor 3	P-glycoprotein	Cancer
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .

HY-17013

Dofequidar 2 Publications Verification MS-209 free base	P-glycoprotein	Cancer
Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-17013D

Dofequidar sesquifumarate MS-209 sesquifumarate	P-glycoprotein	Cancer
Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-159085

P-gp inhibitor 24	P-glycoprotein	Cancer
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-101511

TTT-28	P-glycoprotein	Cancer
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .

HY-17013AR

Dofequidar fumarate (Standard)	P-glycoprotein	Cancer
Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-157876

Anticancer agent 191	P-glycoprotein BCRP	Cancer
Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .

HY-106998

DC-756	Bacterial Antibiotic	Infection
DC-756 is a fluoroquinolone antibiotic. DC-756 possesses potent activity against Gram-positive and Gram-negative pathogens comparable to Trovafloxacin (HY-A0170), with MIC, against Ofloxacin (HY-B0125)-resistant strains 16-fold better than Trovafloxacin. DC-756 is well absorbed orally in rats and found to have good photostability. DC-756 can be used to study bacterial resistance .

HY-149053

OY-101	P-glycoprotein	Cancer
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .

HY-107566

Conessine	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial	Infection Neurological Disease
Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pK_i values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .

HY-U00244A

Benzquinamide hydrochloride P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride	Adrenergic Receptor	Cancer
Benzquinamide (P2647) is an antiemetic which can bind to the α_2A, α_2B, and α_2C adrenergic receptors (α2-AR) with K_i values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .

HY-N0406R

2"-O-beta-L-galactopyranosylorientin (Standard)	Reference Standards Others	Inflammation/Immunology
2"-O-beta-L-galactopyranosylorientin (Standard) is the analytical standard of 2"-O-beta-L-galactopyranosylorientin. This product is intended for research and analytical applications. 2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2). Anti-inflammatory effect .

HY-42034

Hydroquinine Dihydroquinine	Bacterial Parasite Reactive Oxygen Species (ROS) Protein Arginine Deiminase	Infection
Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride .

HY-161260

P-gp inhibitor 20	P-glycoprotein	Cancer
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC₅₀ value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .

HY-107566A

Conessine dihydrobromide	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial	Infection Neurological Disease
Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pK_i values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy .

HY-42034R

Hydroquinine (Standard) Dihydroquinine (Standard)	Reference Standards Bacterial Parasite Reactive Oxygen Species (ROS) Protein Arginine Deiminase	Inflammation/Immunology
Hydroquinine (Standard) is the analytical standard of Hydroquinine. Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride .

HY-W107077

INF55	Bacterial	Infection
INF55 is a NoA multidrug resistance pump inhibitor with the activity of inhibiting the NoA pump. The heterocomplex formed by INF55 combined with berberine shows the potential to combat the resistance of bacterial compounds. INF55 can enhance the antibacterial activity of berberine by reducing its efflux. The structural variants of INF55 can show different NoA inhibitory activities, thereby affecting the antibacterial effect of its corresponding heterocomplexes. Different derivatives of INF55 show similar activity in terms of antibacterial dose and effectiveness .

HY-178111

AcrB-IN-6	Bacterial	Infection
AcrB-IN-6 is an effective AcrB inhibitor. AcrB-IN-6 The compound inhibits the function of bacterial multidrug efflux pumps, thereby significantly enhancing the antibacterial activity of various antibiotics. AcrB-IN-6 achieves 32-fold MIC reductions in wild-type E. coli BW25113. AcrB-IN-6 exhibits excellent synergistic antibacterial effects, low cytotoxicity and hemolytic properties. AcrB-IN-6 can be used for researching anti-resistant bacteria .

HY-172771

Multi-target kinase inhibitor 4	PI3K DNA-PK P-glycoprotein	Cancer
Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .

HY-108694

γ-Tocotrienol 2 Publications Verification	Endogenous Metabolite NF-κB	Metabolic Disease Inflammation/Immunology
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .

HY-108694R

γ-Tocotrienol (Standard)	Reference Standards Endogenous Metabolite NF-κB	Metabolic Disease Inflammation/Immunology
γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .

HY-175838

P-gp-IN-32	P-glycoprotein	Cancer
P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC₅₀ = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .

HY-175522

P-gp-IN-31	P-glycoprotein Apoptosis	Cancer
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 .

HY-144393

P-gp/BCRP-IN-1	BCRP	Cancer
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .

HY-173162

GPV0057	P-glycoprotein Potassium Channel	Cardiovascular Disease Cancer
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-168921

ABCB1-IN-3	P-glycoprotein Apoptosis	Cancer
ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity .

HY-P990196

Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)	P-glycoprotein	Cancer
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-101453

Ceefourin 1	P-glycoprotein	Cancer
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .

Cat. No.	Product Name

HY-L169

Anti-Drug-Resistant Compound Library

539 compounds

Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.

MCE designs a unique collection of 539 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.

Cat. No.	Product Name	Target	Research Area