P-glycoprotein
P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.
Targets for P-glycoprotein
Products for P-glycoprotein
- Cat.No. Product Name Information
- GC60407 (R)-Verapamil D7 hydrochloride (R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
- GC60408 (R)-Verapamil hydrochloride (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
- GC30371 Alisol F Alisol F is a triterpene isolated from Alisma orientalis, has immunosuppressive and anti-virus functions.
- GC12945 Atazanavir An inhibitor of HIV-1 protease
- GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease
- GC64274 AZD-5672 AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM).
- GC33338 Biricodar (VX-710) Biricodar (VX-710) (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
- GC35692 Chrysosplenetin A flavonoid with diverse biological activities
-
GC35727
Coniferyl ferulate
A monolignal conjugate with diverse biological activities
- GC39701 Convallatoxin Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde.
- GC35892 Dofequidar A quinoline derivative and inhibitor of multidrug resistance
- GC13375 Dofequidar fumarate MDR reversal agent
- GC17215 Elacridar An inhibitor of MRP-1 and BCRP
- GC17163 Elacridar hydrochloride An inhibitor of MRP-1 and BCRP
- GC31340 Encequidar (HM30181) Encequidar (HM30181) (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
- GC33185 Encequidar mesylate (HM30181 (mesylate)) Encequidar mesylate (HM30181 (mesylate)) (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
- GC36034 FD 12-9 FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
- GC65385 Ganoderenic acid B Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
- GC10391 Hypophyllanthin P-glycoprotein (P-gp) inhibitor
- GC36345 Isosinensetin Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells.
- GC16609 LY335979 (Zosuquidar 3HCL) Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). LY335979 (Zosuquidar 3HCL) shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.
- GC33375 MCI826 MCI826 is a P-glycoprotein (P-gp) antagonist.
- GC32518 Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) ((±)-Norverapamil hydrochloride ((±)-Norverapamil hydrochloride)), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
- GC18470 NSC 23925 An inhibitor of P-gp
- GC65183 P-gp inhibitor 1 P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
- GC36891 P-gp modulator 1 P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
- GC36855 Paris saponin VII Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
- GN10020 Piperine
- GC33151 Polyoxyethylene stearate (POES) Polyoxyethylene stearate (POES) (POES) is a non-ionic emulsifying agent.
- GN10805 Protopanaxdiol
- GC12523 Reversan inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp)
-
GC12986
Risperidone
SR-2A inhibitor
- GC63175 Roemerine Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
- GC18460 Roquefortine C Roquefortine C is a mycotoxin that was first isolated from a strain of P.
- GC32906 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species.
- GC30033 Sinapine thiocyanate Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
- GC15570 Tariquidar A P-glycoprotein inhibitor
- GC50254 Tariquidar dihydrochloride Potent P-glycoprotein (P-gp) inhibitor
- GC10928 Tariquidar methanesulfonate, hydrate A P-glycoprotein inhibitor
- GC37832 TTT-28 TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
- GC16677 Valspodar A multidrug-resistance modulator
- GC61811 Verapamil Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
- GC45150 Voacamine Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities.
- GC67920 WS-898
- GC65184 YS-370 YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity.
- GC32593 Zamicastat (BIA 5-1058) Zamicastat (BIA 5-1058) (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects.
- GC16672 Zosuquidar A modulator of P-gp