efflux pump

PAβN dihydrochloride (MC-207,110 dihydrochloride) 是一种外排泵抑制剂。

NSC-60339 是一种外排泵抑制剂和 AcrAB-TolC 的底物，是聚对苯二甲酸衍生物，对癌症化疗有潜在作用。

timcodar 是一种非 FKBP12 结合大环内酯衍生物，是外排泵抑制剂，具有抗菌活性，抑制脂质积累，抑制结核杆菌，可用于研究肥胖。

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) 是一种二氢吡啶类钙通道阻滞剂，可抑制细胞外钙离子跨膜流入心肌和血管平滑肌细胞，导致主要冠状动脉和全身动脉扩张，降低心肌收缩力。它常用于心肌功能不全的相关研究。

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) 是一种具有选择性和高效性的 P-糖蛋白药物外排泵抑制剂，具有潜在的抗癌活性，诱导大鼠血脑屏障 P-糖蛋白抑制。

Antibiofilm agent-12（Compound C13）作为一种氨基甲酸酯类衍生的抗真菌剂，对Candida auris表现出突出的抗生物性能。其最小抑菌浓度MIC90达到237.9 μM，能有效抑制Candida auris的药物外排泵活性，并通过促进麦角固醇的耗竭来阻碍其生物膜的形成，并降低其代谢的灵活性。此外，在秀丽隐杆线虫模型中感染Candida auris后，Antibiofilm agent-12同样展现了抗真菌的效果。

Antibacterialagent 269 (3.8) 是抑制肺炎克雷伯菌中AdeG外排泵的活性物质。

NorA-IN-2 (compound DZ-3) 是一种高效的NorA抑制剂，展现了NorA外排泵抑制剂 (EPI) 的活性。

IITR08367 是一种高效的Acinetobacter baumannii Fosfomycin Efflux pump (AbaF) 抑制剂，用于提高Fosfomycin对Acinetobacter baumannii的抗菌效果。其作用机制是干扰Fosfomycin/H+反向转运过程。

Antitrypanosomal agent 24 是一种苯并噻唑偕胺肟，展现出强效且选择性的抗锥虫活性 (IC50 = 0.92 μM)。它是 P-糖蛋白外排泵的底物，并且具有高膜通透性和良好的代谢稳定性。此外，Antitrypanosomal agent 24 通过插入作用与 DNA/RNA 结合。

VEGFR-2/P-gp-IN-1 是一种Licochalcone A 衍生物，具口服活性，作为VEGFR-2 (IC50= 0.885 μM) 和 P-糖蛋白 (P-gp) 的抑制剂。通过同时抑制VEGFR-2激酶活性及P-gp药物外排泵功能，该化合物能够抗肿瘤增殖并克服化疗耐药性。它抑制VEGFR-2和下游PI3K/AKT信号通路蛋白的磷酸化，诱导细胞凋亡并阻滞细胞于S期，同时抑制侵袭性迁移。在HeLa/DDP细胞异种移植瘤模型中，VEGFR-2/P-gp-IN-1 展示出显著的体内抗肿瘤效果，并可用于宫颈癌研究。

FabX-IN-1 (Compound 47) 是一种具有选择性作用的FabX抑制剂，IC50为0.128 μM。其对Helicobacter pylori表现出窄谱抗菌活性，MIC为64 μg/mL。然而，与膜通透剂、外排泵抑制剂及Clarithromycin联合作用时，可显著增强对该菌的抑制效果。FabX-IN-1 可应用于细菌感染研究。

MC-207110 是一种广谱外排泵抑制剂，对铜绿假单胞菌 (P. aeruginosa) 的所有三种已知 Mex 外排泵以及大肠杆菌 (Escherichia coli) 外排泵同源物 (AcrAB-TolC) 均表现出活性。它能够降低铜绿假单胞菌对氟喹诺酮类药物的固有耐药性，适用于感染研究。

Antibacterialagent 309 (Compound C9) 是一种抗菌剂，是AcrB外排泵的底物，能够促进FtsZ聚合。它对耐Erythromycin的S. pyogenes2 (MIC= 0.25 μg/mL)、耐Penicillin的S. aureusCI (MIC= 0.125 μg/mL)、耐Penicillin的S. epidermidis (MIC= 2 μg/mL) 显示出抗菌活性。而对野生型E. coli BW25113 的抗菌活性较弱 (MIC= 256 μg/mL)。

LP07 是一种用于对抗铜绿假单胞菌的抗菌剂，对野生型和外排泵缺陷型P. aeruginosa PA14的最低抑菌浓度（MIC）均为8 μg/mL。其通过直接破坏细菌细胞膜的结构完整性发挥作用。LP07 对MMP-17和MMP-19表现出中等抑制作用，对其他MMP亚型无显著抑制效果。此化合物不影响LpxC酶活性，适用于研究铜绿假单胞菌感染。

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)