p-gp

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

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.

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 (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.

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.

P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that exhibits reverse activity by inhibiting P-gp outflow. P-gb-IN-1 has been shown to inhibit P-gp by hydrogen bonding with residues Asn 721 and Met 986. P-gb-IN-1 showed low toxicity in MCF-7 ADR cells.

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

Tariquidar (XR9576)(Kd=5.1 nM) is a specific and effective non-competitive inhibitor of P-glycoprotein. It can reverse drug resistance in MDR cell Lines.

Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin that exhibits anti-inflammatory and antioxidative effects, offering protection against cardiac hypertrophy.

Bacopaside II is a potential anti-angiogenic agent, it can reduce endothelial cell migration and tubulogenesis and induce apoptosis.

Dihydroevocarpine (1-methyl-2-tridecylquinolin-4-one) induces AML cytotoxicity, apoptosis and G0 G1 blockade, and inhibits tumor growth by inhibiting mTORC1 2 activity and the mTOR pathway in an acute myeloid leukemia (AML) xenograft model.

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 Modulator-5 (compound 25) serves as a modulator of P-gp, effectively inhibiting the proliferation of multidrug-resistant (MDR) tumors. This compound suppresses the function of drug efflux pumps in MDR cells, which results in significant accumulation of ROS and modifications in cell cycle profiles.

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].

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 22 effectively inhibits P-glycoprotein (P-gp) and its efflux function, promoting apoptosis and the accumulation of MCF-7 ADR cells in the S phase [1].

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 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 BCRP-IN-1 (compound 19) is a relatively safe, orally active, and efficient inhibitor of the efflux transporters P-gp and BCRP, which reverses resistance and enhances the oral bioavailability of Paclitaxel (PTX) [1].

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