p-gp inhibitor 1

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

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].

Compound 8a, also known as P-gp inhibitor 14, demonstrates high affinity as a P-gp inhibitor and effectively reverses P-gp-mediated multidrug resistance (EC 50 = 48.74 nM). Additionally, this compound exhibits a weak inhibitory effect on CYP3A4 activity [1].

P-gp Inhibitor 17 (compound 2g), a potent inhibitor, directly interacts with the transmembrane domain of P-gp. This compound is useful for studying P-gp-mediated multidrug resistance in tumor cells [1].

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.

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Polyoxyethylene stearate (POES) is an agent of non-ionic emulsifying.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.

Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.

BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1].

Dofequidar fumarate (MS-209)(MS-209 fumarate), a quinoline-based compound administered orally, is known for counteracting multidrug resistance (MDR) through the inhibition of ABCB1/P-glycoprotein (P-gp) and ABCC1/MDR-associated protein 1.

Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.

TTT-28 is a thiazole-valine peptidomimetic and a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, reversing ABCB1-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.