ABCB1-IN-1 (compound 3) is a potent inhibitor of ABCB1 that promotes cell apoptosis. Featuring 1-benzylimidazole, it exhibits IC50 values of 1.26 μM for Colo205 cells and 2.21 μM for Colo320 cells, respectively [1].

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

Avapritinib (BLU-285) is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).

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

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor. The solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) represents a promising target for the treatment of cancer. MCT1-IN-3 (compound 24) showed the highest MCT1 transport inhibition with an IC50 value of 81.0 Nm. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1.

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.

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.

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

1. Evodine has antinociceptive activity.

Ganoderenic acid B, a natural product derived from Ganoderma lucidum, can work by inhibiting the transport function of ABCB1 and enhancing the cytotoxicity of chemotherapy drugs against AbCB1-mediated multidrug resistant cancer cells.

Epoxylathyrol derivatives have modulation of ABCB1-mediated multidrug resistance in human colon adenocarcinoma and mouse T-Lymphoma cells.

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

Reversin 205 ([Boc-Glu(Obzl)]2-Lys-Ome) serves as an inhibitor of P-glycoprotein (ABCB1) and functions as a peptide chemosensitizer [1].

Wallichinine shows inhibitory activity on platelet aggregation caused by platelet activating factor (PAF). Wallichinine with ABCB1 presents valuable clues for the development of novel MDR reversal reagents from natural products, wallichinine can significa

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

FTY720, an immune modulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.

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

TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocki

Anticancer agent 50 (compound 6) is a potent modulator of the ABCB1 efflux pump with cytotoxic and anti-proliferative activity. anticancer agent 50 reduces the expression of cyclin D1 and induces p53 expression. anticancer agent 50 has shown potential for research in T lymphoma.

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.

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.

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.

WS-691 is a highly Potent and Orally Active ABCB1 Modulator. WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). WS-691 significantly increased the intracellular concentration of PTX and [3H]-PTX while decreasing the efflux of [3H]- PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. WS-691 could stabilize ABCB1 by directly binding to ABCB1 WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vivo without observed toxicity.

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.

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

Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 μM, respectively) but not measles virus or influenza virus (IC50s = >20 μM for both).3

P-gp inhibitor 5 is a potent inhibitor of P-glycoprotein (P-gp), inhibiting P-gp by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. p-gp inhibitor 5 exhibits anti-proliferative effects on some cancer cells. P-gp inhibitor 5 was able to restore cellular sensitivity to Vincristine and Paclitaxel, thereby reversing the multidrug resistant (MDR) phenotype of ABCB1/Flp-InTM-293 and KBvin.

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively).

WS-898 is a potent inhibitor of ABCB1 that reverses resistance to paclitaxel (PTX) in drug-resistant SW620/Ad300, KB-C2 and HEK293/ABCB1 cells with IC50 values of 5.0, 3.67 and 3.68 nM, respectively.

Acerinol is an active ingredient from traditional Chinese medicinal herbs. It could be used as a cancer multidrug resistance reversal agent. Acerinol can significantly stimulate the activity of ABCB1 ATPase without affecting the expression of ABCB1 on nei

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.

Hernandezine is an activator of AMPK activator and a selective reversing agent for ABCB1-mediated MDR in cancer cells.

Efflux inhibitor-1 is a pyrazolopyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC 50 s of 0.45 μM and 2.17 μM, respectively .

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.

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