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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

  1. Cat.No. Product Name Information
  2. 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. (R)-Verapamil D7 hydrochloride  Chemical Structure
  3. 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. (R)-Verapamil hydrochloride  Chemical Structure
  4. GC30371 Alisol F Alisol F is a triterpene isolated from Alisma orientalis, has immunosuppressive and anti-virus functions. Alisol F  Chemical Structure
  5. GC12945 Atazanavir An inhibitor of HIV-1 protease Atazanavir  Chemical Structure
  6. GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease Atazanavir sulfate (BMS-232632-05)  Chemical Structure
  7. GC64274 AZD-5672 AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672  Chemical Structure
  8. 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. Biricodar (VX-710)  Chemical Structure
  9. GC35692 Chrysosplenetin A flavonoid with diverse biological activities Chrysosplenetin  Chemical Structure
  10. GC35727 Coniferyl ferulate

    A monolignal conjugate with diverse biological activities

    Coniferyl ferulate  Chemical Structure
  11. GC39701 Convallatoxin Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin  Chemical Structure
  12. GC35892 Dofequidar A quinoline derivative and inhibitor of multidrug resistance Dofequidar  Chemical Structure
  13. GC13375 Dofequidar fumarate MDR reversal agent Dofequidar fumarate  Chemical Structure
  14. GC17215 Elacridar An inhibitor of MRP-1 and BCRP Elacridar  Chemical Structure
  15. GC17163 Elacridar hydrochloride An inhibitor of MRP-1 and BCRP Elacridar hydrochloride  Chemical Structure
  16. GC31340 Encequidar (HM30181) Encequidar (HM30181) (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. Encequidar (HM30181)  Chemical Structure
  17. GC33185 Encequidar mesylate (HM30181 (mesylate)) Encequidar mesylate (HM30181 (mesylate)) (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor. Encequidar mesylate (HM30181 (mesylate))  Chemical Structure
  18. 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. FD 12-9  Chemical Structure
  19. 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. Ganoderenic acid B  Chemical Structure
  20. GC10391 Hypophyllanthin P-glycoprotein (P-gp) inhibitor Hypophyllanthin  Chemical Structure
  21. GC36345 Isosinensetin Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin  Chemical Structure
  22. 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. LY335979 (Zosuquidar 3HCL)  Chemical Structure
  23. GC33375 MCI826 MCI826 is a P-glycoprotein (P-gp) antagonist. MCI826  Chemical Structure
  24. 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. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride)  Chemical Structure
  25. GC18470 NSC 23925 An inhibitor of P-gp NSC 23925  Chemical Structure
  26. GC65183 P-gp inhibitor 1 P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. P-gp inhibitor 1  Chemical Structure
  27. 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). P-gp modulator 1  Chemical Structure
  28. 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. Paris saponin VII  Chemical Structure
  29. GN10020 Piperine Piperine  Chemical Structure
  30. GC33151 Polyoxyethylene stearate (POES) Polyoxyethylene stearate (POES) (POES) is a non-ionic emulsifying agent. Polyoxyethylene stearate (POES)  Chemical Structure
  31. GN10805 Protopanaxdiol Protopanaxdiol  Chemical Structure
  32. GC12523 Reversan inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp) Reversan  Chemical Structure
  33. GC12986 Risperidone

    SR-2A inhibitor

    Risperidone  Chemical Structure
  34. 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. Roemerine  Chemical Structure
  35. GC18460 Roquefortine C Roquefortine C is a mycotoxin that was first isolated from a strain of P. Roquefortine C  Chemical Structure
  36. GC32906 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine  Chemical Structure
  37. 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. Sinapine thiocyanate  Chemical Structure
  38. GC15570 Tariquidar A P-glycoprotein inhibitor Tariquidar  Chemical Structure
  39. GC50254 Tariquidar dihydrochloride Potent P-glycoprotein (P-gp) inhibitor Tariquidar dihydrochloride  Chemical Structure
  40. GC10928 Tariquidar methanesulfonate, hydrate A P-glycoprotein inhibitor Tariquidar methanesulfonate, hydrate  Chemical Structure
  41. 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. TTT-28  Chemical Structure
  42. GC16677 Valspodar A multidrug-resistance modulator Valspodar  Chemical Structure
  43. GC61811 Verapamil Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil  Chemical Structure
  44. GC45150 Voacamine Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities. Voacamine  Chemical Structure
  45. GC67920 WS-898 WS-898  Chemical Structure
  46. 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. YS-370  Chemical Structure
  47. 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. Zamicastat (BIA 5-1058)  Chemical Structure
  48. GC16672 Zosuquidar A modulator of P-gp Zosuquidar  Chemical Structure

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