P-gp

Valspodar (PSC 833), a specific P-glycoprotein inhibitor and MDR regulator, is commonly used as a chemical sensitizer in the study of advanced epithelial ovarian cancer.

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

HTT-D3 is an orally active, highly efficient Huntington splicing modulator. It induces HTT mRNA degradation, reduces HTT protein levels, and inhibits P-glycoprotein (P-gp) efflux. This compound can be used in Huntington's disease research.

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

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.

MCI826 is a potent and selective antagonist of P-glycoprotein (P-gp) and peptide leukotrienes (p-LTs), showing anti-asthmatic activity in a guinea pig model of advanced asthma.

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.

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

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.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu

Chrysosplenetin is a metabolic inhibitor of artemisinin.

Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.

Zosuquidar (RS 33295-198) is a potent P-glycoprotein inhibitor with antitumor activity, inhibits tumor growth, significantly inhibits PD-L1 expression by triggering its autophagic degradation, and is used in the study of acute myeloid leukemia.

Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode

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

Agnuside (chasteberry oil) inhibits COX-2 (IC50: 0.026 mg ml) but exhibits less than 10% inhibition of COX-1 at this concentration. It also inhibits 46.3, 66.8, and 82.1% of P-glycoprotein (P-gp) ATPase activity at concentrations of 5, 25, and 100 μM, respectively.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

Encequidar (HM30181A) is a potent and selective P-glycoprotein inhibitor.

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

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

(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) (20-Epiprotopanaxadiol), an apoptosis inducer, is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin.

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

Taxol C can reduce interaction with the P-glycoprotein transporter that may allow for increased permeation of taxanes into the brain.

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

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.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

Coniferyl ferulate is a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis. It shows strong inhibition of human placental GST (IC50: 0.3 μM). It also reverses multidrug resistance and downregulates P-glycoprotein.

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.

Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800). It is also a phenolic-chloine conjugates, acting as anti-oxidants and acetylcholinesterase inhibitors, that can be used for the treatment of Alzheimer's disease (AD).

1. Sinapine, an alkaloid from seeds of the cruciferous species, can be used as an effective natural compound for chemo-resistance. 2. Sinapine has antioxidant and radio-protective activities.

Convallatoxin is a natural product

Alisol F 24-acetate, a natural product isolated from Alisma plantago-aquatica Linn[1], enhances chemosensitivity and apoptosis of MCF-7 DOX Cells by inhibiting P-Glycoprotein-Mediated drug efflux[2].

YS-370 is an orally active inhibitor of P-gp and shows moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance to paclitaxel and colchicine and exhibits stronger antitumor activity in combination with paclitaxel.

Pristinamycin IA (Mikamycin B) is a cyclo-peptidic macrolactone antibiotic and a substrate for the P-glycoprotein.

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.

HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs.

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.

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

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.

Larotaxel (XRP9881) is a taxane analogue with anticancer activity that promotes tubulin assembly and stabilizes microtubules, inducing apoptosis. It crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, making it useful for studying breast and bladder cancer.

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

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

Tenacissoside G is a C21 steroid from the stem of Marsdenia tenacissima. It reverses multidrug resistance in multidrug-resistant cancer cells overexpressing P-glycoprotein.

1. Isosinensetin (6-Demethoxynobiletin) shows antioxidant and HIV-1 protease inhibiting activities.

Furanodiene has anti-inflammatory and antioxidant activities, it is active against gram-positive bacteria and Candida albicans.

Hypophyllanthin and phyllanthin have antitumour effects against Ehrlich Ascites Carcinoma in mice.

Euphorbia factor L1 (Euphorbiasteroid) can reduce Bcl-2, PI3K, AKT, and mTOR protein and mRNA levels, and up-regulate caspase-9 and caspase-3 protein levels. It induces autophagy and has anti-cancer, anti-adipogenic, anti-osteoclastogenic, and multidrug-resistant regulatory effects.