PGP-4008 is a selective and potent P-glycoprotein (Pgp) inhibitor that inhibits tumor growth by co-administration with Doxorubicin.

Penicillin G Procaine is a β-lactam antibiotic and is a crystalline complex produced by chemically combining penicillin G with procaine.

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

5'-pGpG is a linearized form of cyclic di-GMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3It is a metabolite of cyclic di-GMP formedviahydrolysis by various phosphodiesterases (PDEs) that binds to the cyclic di-GMP-I riboswitch with reduced affinity compared to cyclic di-GMP.4,55'-pGpG is intended for use as a negative control for cyclic di-GMP signaling.

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

M7GpppGpG, a trinucleotide cap analogue and oligonucleotide, protects against premature degradation by 5′-exonucleases and facilitates pre-mRNA splicing, mRNA transport, and protein biosynthesis initiation by recruiting essential proteins [1].

PGPC (1-Palmitoyl-2-glutaryl phosphatidylcholine) is an oxidized phospholipid and activates peroxisome proliferator-activated receptor in a concentration-dependent manner.

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

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

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 (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.

Pepluanin A, shows a very high activity for a jatrophane diterpene, outperforming cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated daunomycin transport.

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

1. Evodine has antinociceptive activity.

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

Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.

(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs.

ST7710AA1 is a PARP-1 inhibitor that acts by showing significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp.

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

BNC105P is a benzofuran-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and antineoplastic activities. Upon administration vascular disrupting agent BNC105P, the disodium phosphate ester of BNC105, is rapidly converted to BNC105; in activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may result in a blockage of mitotic spindle formation, cell cycle arrest, and disruption of the tumor vasculature. Hypoxic conditions ensue, depriving tumor cells of nutrients and resulting in tumor cell apoptosis. In addition to its VDA activity, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization. BNC105 is not a substrate for the multidrug-resistance P-glycoprotein (Pgp) transporter.

Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is the first natural product steroid identified to have these cellular effects,with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.

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.

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.

NSC23925 is a selective and effective inhibitor of P-glycoprotein (Pgp).

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

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].

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.

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).

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

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

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.

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.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.

BACE1/2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 has lower Pgp efflux ratio and improved passive permeability. The metabolic stability of BACE1/2-IN-1 in liver microsomes is decreased.

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

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

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

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

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

Convallatoxin is a natural product

Clerosterol ((-)-Clerosterol) is a small molecule compound derived from Roasted bupleuri in vinegar that inhibits Pgp overexpression. Clerosterol shows cytotoxicity to human melanoma cells and can be used to study the loss of mitochondrial membrane potential.

NSC-57969 is a MDR-selective agent, exhibiting a robust Pgp-dependent toxic activity across diverse cancer cell lines.

Deoxynivalenol (Vomitoxin) is a mycotoxin produced by Fusarium spp. of the single trichothecene family and is commonly found in contaminated food and feed.Deoxynivalenol crosses the intestinal mucosa via a cellular bypass at the tight junctions.Deoxynivalenol transporters are unaffected by inhibitors of P-glycoprotein (PgP) or multidrug resistance-associated protein (MRP). Deoxynivalenol commonly causes diarrhea, vomiting, and gastrointestinal inflammation in humans and animals.

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.

Reversan is a potent and nontoxic multidrug inhibitor of resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp).

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

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.

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