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.

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

INF55 inhibits NorA efflux pump.

SLUPP-225 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.

SLUPP-417 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

Anticancer agent 50 (compound 6), a potent modulator of the ABCB1 efflux pump, exhibits cytotoxic and anti-proliferative activity by reducing cyclin D1 expression and inducing p53 expression. It shows significant potential for research in T lymphoma.

Dexverapamil is the R-enantiomer of the calcium channel blocker verapamil. Dexverapamil competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms.

Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites was originally isolated from the myxobacterium Solangium cellulosum.

Cabazitaxel-d6 is a deuterium labeled cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes 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, this agent is a poor substrate for the membrane-associated, multidrug resistance (MDR), P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. In addition, cabazitaxel penetrates the blood-brain barrier (BBB).