Membrane Transporters-Ion Channels

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  1. CFTR inhibitor

    PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.
  2. TRPC1/4/5 channels inhibitor

    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  3. myosin II inhibitor

    Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
  4. MCT Inhibitor?€?

    7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  5. a-K-ATPase inhibitor

    Ouabain is a selective Na+, K+-ATPase inhibitor.
  6. CFTR inhibitor

    CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).
  7. CFTR inhibitor

    CFTRinh-172 is a voltage-independent, selective CFTR inhibitor
  8. Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
  9. sodium-potassium pump inhibitor

    Digoxin is a sodium-potassium pump inhibitor.
  10. Sodium Channel inhibitor

    AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
  11. LAT-1 inhibitor

    JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor.
  12. TRPC3 inhibitor

    Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.
  13. P-gp & BCRP inhibitor

    Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.
  14. MCT1 inhibitor

    AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
  15. VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
  16. P-gp inhibitor

    Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.
  17. MCT1 and MCT2 inhibitor

    AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.
  18. ATPase inhibitor

    Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells.
  19. Calcium Channel inhibitor

    Nimodipine is a L-type Ca2+ channel blocker.
  20. TRPP3 channel inhibitor

    EIPA (L593754; MH 12-43) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA (L593754; MH 12-43) also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
  21. MSCs Inhibitor

    GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.
  22. MDR1/P-gp Inhibitor

    PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
  23. SGLT1/SGLT2 inhibitor

    Phlorizin is a competitive inhibitor of SGLT1 and SGLT2; this reduces renal glucose transport, lowering the amount of glucose in the blood.
  24. ATPase inhibitor

    Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.
  25. NHE3 inhibitor

    Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.
  26. CHC

    MCT inhibitor

    CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.
  27. SGLT2 inhibitor

    Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.
  28. HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
  29. SGLT2 inhibitor

    Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.
  30. NCX inhibitor

    SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger with IC50 of 5-33 nM (inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia).
  31. SGLT2 Inhibitor

    Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).
  32. CRM1 inhibitor

    KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
  33. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  34. BCRP inhibitor

    Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM.
  35. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  36. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  37. Proton Pump inhibitor

    Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion.
  38. Na+/Ca2+ Exchanger Inhibitor

    KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.
  39. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  40. Nav inhibitor

    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  41. Ca2+ channel agonist/CDK2 inhibitor

    Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  42. P-gp inhibitor

    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.
  43. Pgp1 inhibitor

    NSC 23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1).
  44. NHE-1 inhibitor

    Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).
  45. BCRP/ABCG2 inhibitor

    YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2).
  46. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  47. TRPC6 inhibitor

    SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
  48. proton pump inhibitor

    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
  49. H(+)-K(+)-exchanging ATPase inhibitor

    Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.
  50. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.

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