p-gp

P-gp modulator 1 is a high-affinity, orally available P-glycoprotein (Pgp) modulator.

P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562/A02 cells).

P-gp modulator 2 (Compound 27) is a potent competitive and metabotropic modulator of P-glycoprotein (P-gp).

P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor, reducing P-gp activity by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. It exhibits anti-proliferative effects on certain cancer cells and restores cellular sensitivity to Vincristine and Paclitaxel, reversing the multidrug resistant (MDR) phenotype of ABCB1/Flp-InTM-293 and KBvin.

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

P-gp Inhibitor 3, an effective P-glycoprotein (P-gp) inhibitor, activates P-gp ATPase to inhibit P-gp's efflux function. It demonstrates a relatively stronger multidrug resistance (MDR) reversal ability, thereby enhancing the anti-tumor efficacy of Paclitaxel.

P-gp inhibitor 4 is a selective P-glycoprotein modulator with an EC 50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

P-gp Inhibitor 2 is a powerful P-glycoprotein (P-gp) inhibitor, effective in reversing Doxorubicin resistance with an IC50 of 0.22 µM in human colorectal carcinoma cells overexpressing P-gp (SW600 Ad300).

P-gp Inhibitor 13, a P-glycoprotein antagonist, can counteract paclitaxel resistance in A2780/T cells, proving valuable for advanced acute myeloid leukemia research [1].

P-gp Inhibitor 15 (compound 7a), a nonsubstrate inhibitor of P-glycoprotein (Pgp), inhibits Pgp-ATPase activity and interferes with Pgp-mediated Rhodamine123 efflux. Additionally, this compound enhances the inhibitory effect of Paclitaxel on tumor progression in the KBV xenograft tumor model in nude mice [1].

P-gp/BCRP-IN-2 (compound 15), an oxadiazole derivative, functions as a dual inhibitor targeting both the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). Additionally, it bolsters the anti-proliferative impact of Doxorubicin in the drug-resistant HT29/DX and MDCK-MDR1 human adenocarcinoma colon cancer cell lines [1].

P-gp-IN-30 (Compound 13) is an inhibitor of P-glycoprotein (P-gp) that targets YB-1. It reduces the expression of total YB-1 protein and nuclear YB-1 protein, thereby inhibiting the expression and function of downstream P-gp, which significantly enhances sensitivity to paclitaxel by inhibiting its efflux rate. When combined with paclitaxel, P-gp-IN-30 effectively suppresses tumor growth in A549/Taxol xenograft mouse models. This compound is useful for research on non-small cell lung cancer (NSCLC).

P-gp Inhibitor 25 (compound 16c) is a P-gp inhibitor that enhances the oral absorption of paclitaxel. It is utilized in cancer research to improve treatment efficacy.

P-gp inhibitor 27 (Compound D2) is an inhibitor of P-glycoprotein (P-gp) that reduces the expression of P-gp and MRP1. It increases the accumulation of Rh123 in A2780/T cells and reverses multidrug resistance to Paclitaxel (EC50 of 88 nM) and Cisplatin.

Lysosomal P-gp targeted agent 1 (Compound 14) is an antitumor drug that targets lysosomal P-glycoprotein (Pgp). It is selectively transported to lysosomes via overexpressed Pgp, releasing nitric oxide that generates reactive oxygen species (ROS), causing lysosomal membrane permeabilization (LMP) and inducing apoptosis. This compound can overcome resistance mediated by P-glycoprotein, leading to cell cycle arrest while maintaining relatively low toxicity to normal cells. It exhibits antitumor activity by significantly inhibiting tumor growth.

P-gp inhibitor 28 (Compound 4h) is an inhibitor of P-glycoprotein (P-gp) that can suppress cancer cell proliferation, with an IC50 value ranging from 15.88 to 21.96 μM in MCF-7/ADR cells. This compound enhances the accumulation of Rho123 in MCF-7/ADR cells and is applicable for research in cancer treatment and overcoming tumor multidrug resistance.

P-gp inhibitor 29 (41) is a potent inhibitor of P-gp and an apoptosis inducer, with an IC50 value of 8.9 nM in Eca109/VCR cells, making it useful for esophageal cancer research.

P-gp modulator-7 (Compound 9e) is an inhibitor of P-glycoprotein (P-gp). It uniquely occupies the channel entrance of P-gp in a T-shaped conformation, blocking the peristaltic extrusion mechanism of transmembrane domains TM12 and TM9. This action inhibits P-gp from pumping drugs out of cells and reverses multidrug resistance (MDR) in tumor cells. P-gp modulator-7 shows promise for cancer research.

P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.

P-gp inhibitor 18 (compound 6G) effectively inhibits P-gp, reducing the efflux of Rhodamine 123 in P-gp overexpressing leukemia cells, such as K562/Dox.

P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor that blocks the efflux of rhodamine 123 from P-gp overexpressing leukemia cells K562/Dox and restores the sensitivity of DOX-resistant cells.

P-gp inhibitor 20 (Compound H27) is a P-glycoprotein (P-gp) inhibitor characterized by low cytotoxicity. It reverses multidrug resistance (MDR) in MCF-7/ADR cells by inhibiting the efflux function of P-gp in a dose-dependent manner without affecting P-gp expression, with an IC50 value of 46.6 nM. P-gp inhibitor 20 is suitable for cancer research.

P-gp inhibitor 23 (compound 14F) is an effective inhibitor of both P-gp and CYP3A4, with an EC50 of 28 nM for P-gp and an IC50 of 223 nM for CYP3A4.

P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). This compound demonstrates multidrug resistance (MDR) reversal activity in cancer, with an IC50 for Paclitaxel of 8.80 and a reversal fold of 211.8.