efflux pump

By Targets:	5-HT Receptor (1) ADC Cytotoxin (1) Antibiotic (4) Bacterial (15) Biochemical Assay Reagents (1) Calcium Channel (3) Dopamine Receptor (1) Drug Metabolite (3) Fungal (1) MDM-2/p53 (1) P-glycoprotein (5) Parasite (3) Topoisomerase (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (3) Infection (20) Inflammation/Immunology (3) Neurological Disease (1)

Targets Recommended: Proton Pump Na+/K+ ATPase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-Y1777

2-Phenylacetophenone	Others	Infection
2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .

HY-149811

AcrB-IN-3	Bacterial Parasite	Infection
Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .

HY-149812

AcrB-IN-4	Bacterial Parasite	Infection
Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .

HY-149810

AcrB-IN-2	Bacterial Parasite	Infection
AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .

HY-156753

NorA-IN-1	Others	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-N2947

Boeravinone B	P-glycoprotein	Infection Inflammation/Immunology
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-101444A

PAβN dihydrochloride Maximum Cited Publications 6 Publications Verification MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride	Bacterial	Infection
PAβN dihydrochloride (MC-207110 dihydrochloride) is an **efflux pump** inhibitor.

HY-124819

D13-9001	Bacterial	Infection
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the K_D values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .

HY-157533

AcrB-IN-5

Bacterial Others

AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .

AcrB-IN-5	Bacterial	Others
AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .

HY-119172

NSC-60339	Bacterial	Infection Inflammation/Immunology Cancer
NSC-60339, an **efflux pump** inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent .

HY-163454

NorA-IN-2

Bacterial Infection

NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .

NorA-IN-2	Bacterial	Infection
NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .

HY-157987

MBX3135	Bacterial	Infection
MBX3135 is an efflux pump inhibitor which can enhance the effect of antibiotics through the AcrB target of bacteria. MBX3135 can be used for research of infection and antibiotics .

HY-162144

BDM91288	Bacterial	Infection
BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .

HY-155048

BDM91270	Bacterial	Infection
BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC₉₀ of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .

HY-17390A

Loxapine succinate	5-HT Receptor Dopamine Receptor	Infection Neurological Disease
Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .

HY-100750

Norverapamil hydrochloride 1 Publications Verification (±)-Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
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 .

HY-135328

Norverapamil (±)-Norverapamil; D591	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-120574

TH1338	ADC Cytotoxin Topoisomerase	Cancer
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .

HY-146389

Anticancer agent 50	MDM-2/p53 P-glycoprotein	Cancer
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 .

HY-N10069

Bonducellin	Others	Infection
Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of **efflux pump** (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .

HY-N12320

Majoranaquinone	Antibiotic	Infection
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .

HY-135328S

Norverapamil-d7 (±)-Norverapamil-d₇; D591-d₇	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
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[1][2].

HY-155198

Antifungal agent 72	Fungal	Infection
Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (K_i: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .

HY-P1649B

SPR741 acetate 2 Publications Verification NAB741 acetate	Bacterial Antibiotic	Infection
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .

HY-P1649

SPR741 NAB741	Bacterial Antibiotic	Infection
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .

HY-P1649A

SPR741 TFA NAB741 TFA	Bacterial Antibiotic	Infection
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .

HY-N4314

Scutellarein tetramethyl ether 1 Publications Verification 4',5,6,7-Tetramethoxyflavone	Bacterial	Infection Inflammation/Immunology
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial agent resistance via efflux pump inhibition . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation .

HY-W127487

N-Octadecanoyl-L-homoserine lactone	Biochemical Assay Reagents	Others
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.

Cat. No.	Product Name

HY-L048

Antifungal Compound Library	343 compounds
The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins, overexpression and changes in drug targets and biofilm formation, emphasizing the importance of discovering new antifungal drugs and therapies. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, such as the combination of antifungal drugs, development of new formulations for antifungal agents and modifications to the chemical structures of traditional antifungals, etc. MCE offers a unique collection of 343 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.

Antifungal Compound Library

343 compounds

The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins, overexpression and changes in drug targets and biofilm formation, emphasizing the importance of discovering new antifungal drugs and therapies. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, such as the combination of antifungal drugs, development of new formulations for antifungal agents and modifications to the chemical structures of traditional antifungals, etc.

MCE offers a unique collection of 343 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.

Cat. No.	Product Name	Type

HY-W127487

N-Octadecanoyl-L-homoserine lactone	Biochemical Assay Reagents
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.

N-Octadecanoyl-L-homoserine lactone

Biochemical Assay Reagents

Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.

Cat. No.	Product Name	Target	Research Area

HY-P1649B

SPR741 acetate 2 Publications Verification NAB741 acetate	Bacterial Antibiotic	Infection
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .

HY-P1649

SPR741 NAB741	Bacterial Antibiotic	Infection
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .

HY-P1649A

SPR741 TFA NAB741 TFA	Bacterial Antibiotic	Infection
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2947

Boeravinone B	Natural Products other families Classification of Application Fields Source classification Phenols Polyphenols Plants Disease Research Fields Inflammation/Immunology	P-glycoprotein
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-N4314

Scutellarein tetramethyl ether 1 Publications Verification 4',5,6,7-Tetramethoxyflavone	Infection Structural Classification Flavonoids Classification of Application Fields Flavones Plants Compositae Inflammation/Immunology Disease Research Fields Genista maderensis (Webb & Berthel.) Lowe	Bacterial
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial agent resistance via efflux pump inhibition . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation .

HY-N10069

Bonducellin	Structural Classification Flavonoids Leguminosae Caesalpinia sappan L. Source classification Plants Other Flavonoids	Others
Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of **efflux pump** (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .

HY-N12320

Majoranaquinone	Quinones Structural Classification Labiatae Source classification Origanum majorana L. Plants Naphthalene Quinones	Antibiotic
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .

Cat. No.	Compare	Product Name	Species	Source

HY-P702268

	Efflux pump membrane transporter Protein, Acinetobacter baumannii (Cell-Free, His) efflux pump membrane transporter	Others	E. coli Cell-free
	Efflux pump membrane transporters are part of the Resistant Nodule Cell Division (RND) family and play a critical role in the efflux of multiple substrates across the cell membrane. As a member of this family, it has conserved characteristics that underline its importance in cellular transport. Efflux pump membrane transporter Protein, Acinetobacter baumannii (Cell-Free, His) is the recombinant Efflux pump membrane transporter protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of Efflux pump membrane transporter Protein, Acinetobacter baumannii (Cell-Free, His) is 1036 a.a., with molecular weight of 114.2 kDa.


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Cat. No.	Product Name	Chemical Structure

HY-135328S

Norverapamil-d7
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[1][2].

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Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

efflux pump

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

NaturalProducts

Recombinant Proteins

Isotope-Labeled Compounds

Natural
Products