efflux pump

PAβN dihydrochloride (MC-207,110 dihydrochloride) is an inhibitor of efflux pump.

NSC-60339 is an inhibitor of efflux pump, and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent.

timcodar is a non-FKBP12 binding macrolide derivative that is an efflux pump inhibitor with antimicrobial activity, inhibition of lipid accumulation, inhibition of Mycobacterium tuberculosis, and can be used in the study of obesity. timcodar is a non-FKBP12 binding macrolide derivative with antimicrobial activity.

Thalicarpine is a natural aporphine benzylisoquinoline vinca alkaloid with antineoplastic activity. Thalicarpine binds to and inhibits p-glycoprotein, the multidrug resistance efflux pump. Thalicarpine also induces single-strand breaks in DNA and arrests cancer cells at the G2/M and G1 phase of the cell cycle. Check for active clinical trials or closed clinical trials using this agent.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

The KD values of D13-9001 in Escherichia coli and Pseudomonas aeruginosa were 1.15μM and 3.57μM, respectively. D13-9001 has antibiotic activity. It is an effective AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor.

Tariquidar methanesulfonate hydrate (XR9576 methanesulfonate hydrate) is a selective and potent P-glycoprotein drug efflux pump inhibitor with potential anticancer activity that induces P-glycoprotein inhibition of the blood-brain barrier in rats.

Antibiofilm agent-12 (Compound C13), an antifungal belonging to the carbamate derivatives, exhibits significant antifungal activity against Candida auris, with an MIC90 of 237.9 μM. It inhibits the drug efflux pump activity of Candida auris and promotes ergosterol depletion, thereby hindering the formation of Candida auris biofilms and reducing its metabolic flexibility. Additionally, Antibiofilm agent-12 demonstrates antifungal efficacy in a C. elegans model following Candida auris infection.

Antibacterialagent 269 (3.8) acts as an inhibitor of the AdeG efflux pump in Klebsiella pneumoniae.

NorA-IN-2 (compound DZ-3) is a potent inhibitor of NorA. It exhibits activity as a NorA efflux pump inhibitor (EPI).

IITR08367 is a potent inhibitor of the efflux pump Acinetobacter baumannii Fosfomycin Efflux pump (AbaF), designed to enhance the antibacterial activity of Fosfomycin against Acinetobacter baumannii. It operates by disrupting the Fosfomycin/H+ antiport activity.

Antitrypanosomal agent 24 is a benzothiazole amidoxime compound with potent and selective activity against trypanosomes (IC50 = 0.92 μM). It serves as a substrate for the P-glycoprotein efflux pump and exhibits high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA via intercalation.

VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.

FabX-IN-1 (Compound 47) is a selective FabX inhibitor with an IC50 of 0.128 μM. It exhibits narrow-spectrum antibacterial activity against Helicobacter pylori, with an MIC of 64 μg/mL. Its synergistic inhibitory effect is significantly enhanced when used in combination with membrane-permeabilizing agents, efflux pump inhibitors, and Clarithromycin. FabX-IN-1 is applicable for bacterial infection research.

MC-207110 is a broad-spectrum efflux pump inhibitor. It is effective against all three known Mex efflux pumps in Pseudomonas aeruginosa (P. aeruginosa) and their homologous counterparts (AcrAB-TolC) in the closely related Escherichia coli. MC-207110 reduces the intrinsic resistance of Pseudomonas aeruginosa to fluoroquinolone antibiotics and is useful for research in infections.

Antibacterialagent 309 (Compound C9) is an antibacterial agent that serves as a substrate for the AcrB efflux pump. It promotes the polymerization of FtsZ and exhibits antibacterial activity against erythromycin-resistant S. pyogenes2 (MIC = 0.25 μg/mL), penicillin-resistant S. aureusCI (MIC = 0.125 μg/mL), and penicillin-resistant S. epidermidis (MIC = 2 μg/mL). However, it shows weak antibacterial activity against wild-type E. coli BW25113 (MIC = 256 μg/mL).

LP07 is an antibacterial agent targeting Pseudomonas aeruginosa. It exhibits a minimum inhibitory concentration (MIC) of 8 μg/mL against both wild-type and efflux pump-deficient strains of P. aeruginosa PA14. LP07 exerts its antibacterial effects by directly disrupting the structural integrity of bacterial cell membranes. It shows moderate inhibition of MMP-17 and MMP-19 but has no significant inhibitory effect on other MMP subtypes. LP07 does not inhibit LpxC enzyme activity and can be utilized in research on Pseudomonas aeruginosa infections.

PA36-2 is an Mdr1 inhibitor and an azole resistance reversal agent, exhibiting an IC50 of 1.0 μg/mL and a Kd of 4.209 μM against Candida albicans Mdr1. By effectively inhibiting the activity of the Mdr1 efflux pump, PA36-2 prevents the expulsion of substrates from cells, thereby enhancing the intracellular accumulation of azole antibiotics. This compound can act synergistically with antifungals such as Fluconazole (FLC) and is useful for research on azole-resistant candidiasis.

Premafloxacin is a potent antimicrobial agent effective against Staphylococcus aureus, Corynebacterium bovis, and Amycolatopsis orientalis. It exhibits strong antibacterial activity against S. aureus by targeting topoisomerase IV (topoisomeraseIV) and is a weak substrate of the NorA efflux pump. Premafloxacin can be utilized in antimicrobial research.

Antibioticadjuvant 4 (Compound 13) is an antibiotic adjuvant and efflux pump inhibitor. It exhibits strong inhibitory effects on efflux pumps. When used alone or in combination with antibiotics, Antibioticadjuvant 4 significantly downregulates virulence-associated genes in Staphylococcus aureus. Additionally, it enhances the efficacy of Ciprofloxacin against multidrug-resistant Staphylococcus aureus strains.

ATMpotentiator-1 (compound 9) acts as a β-lactamase inhibitor and efflux pump inhibitor with an IC50 of 1.6 μM for NDM-1, 12.5 μM and 5.4 μM for OXA-10, 5.0 μM for VIM-2, 26.7 μM for KPC-2, and 3.4 μM for OXA-48. It inhibits efflux pump activity in *Pseudomonas aeruginosa* and shows synergistic inhibitory effects when used with CCCP. ATMpotentiator-1 is applicable in research on carbapenem-resistant *Pseudomonas aeruginosa* (CRPA) infections.

MCC1189 is a first-in-class MFS efflux pump CaMdr1p inhibitor.

DS-8587 is a DNA topoisomerase inhibitor. DS-8587 exhibits potent antibacterial activity against quinolone-resistant A. baumannii isolates that harbor mutations in quinolone resistance-determining regions. DS-8587 significantly reduces the number of viabl