P-gp

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

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

Tepotinib hydrochloride(1 : x) is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations.

Laniquidar TFA (R101933) is a novel orally available non-competitive P-glycoprotein (P-gp) inhibitor with an IC50 value of 0.51 μM.Laniquidar has limited bioavailability and can be used to modulate the multidrug resistance transporter.Laniquidar can be used for the study of AML and myelodysplastic syndrome (MDS). Laniquidar is used to study acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).

FM04 is an orally active and highly potent inhibitor of P-glycoprotein (P-gp) with an EC50 value of 83 nM. FM04 can interact with Q1193 and I1115 in human P-gp nucleotide binding domain 2 (NBD2). Thereby disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling the ICL2-NBD2 interaction, thereby inhibiting P-gp. FM04 can be used in the treatment of cancer and tumors.

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

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.

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

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.

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

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

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

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.

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

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

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

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.

Cinchonine (LA40221), a local anesthetic of the amide type, now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local narcotics and its parenteral use is restricted to spinal anesthesia.

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.

Jatrophane 5 demonstrates the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-TxR).

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

Lappaol C has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol C also has potential chemosensitizing activity, it may be candidates for developing novel adjuvant an

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.

Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.

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.

1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade.
2. Lappaol F has potential chemosensitizing activity, it may be candidates for developing novel adju

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.

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

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

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

(-)-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.

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.

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

Larotaxel (XRP9881) is a taxane analogue that has anticancer activity, exerts its cytotoxic effects by promoting tubulin assembly and stabilizing microtubules, and ultimately induces cell death through apoptosis. Larotaxel (XRP9881) is a compound that crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, which can be used to study breast and bladder cancer.

Pafenolol is a P-glycoprotein modulator with a Ki value of 5.5 µM. pafenolol is an orally available and selective beta-adrenergic receptor antagonist.

Taxuspine X may have p-glycoprotein inhibitory activity.

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

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

7β-Hydroxylathyrol is a diterpenoid extract from the seed oil of Caper Spurge and displays P-gp inhibition resulting in cytotoxic properties.

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.

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

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).

2,5,7,8,9,14-Hexaacetoxy-3-benzoyloxy-15-hydroxyjatropha-6(17),11E-diene (Jatrophane 2 ) exhibits significant antifeedant activity against a generalist plant-feeding insect, the cotton bollworm (Helicoverpa armigera). Jatrophane 2 also demonstrates the mo

Chrysosplenetin is a metabolic inhibitor of artemisinin.

Valspodar (PSC 833) is a specific P-glycoprotein inhibitor and MDR regulator often used as a chemical sensitizer to study advanced epithelial ovarian cancer.

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

AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM. AZD-5672 inhibits hERG cardiac ion channel binding and P-gp-mediated digoxin transport with IC50s of 7.3 μM and 32 μM. AZD-5672 can be used in studies about rheumatoid arthritis.