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Results for "

P-glycoprotein

" in MCE Product Catalog:

98

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

22

Natural
Products

1

Recombinant Proteins

11

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas
  • HY-15134
    ONT-093

    OC 144-093; OC 144093

    		 P-glycoprotein Cancer
    ONT-093 is a potent inhibitor of P-glycoprotein pump. ONT-093 has the potential for the research cancer diseases.
  • HY-A0279A
    Pristinamycin IA

    Mikamycin B; Mikamycin IA

    		 Bacterial Antibiotic Infection
    Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus.
  • HY-50879
    Elacridar

    GF120918; GW0918; GG918; GW120918

    		 P-glycoprotein BCRP Cancer
    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on drug distribution to brain and the research of cancer.
  • HY-119823
    PGP-4008

    		P-glycoprotein Cancer
    PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin.
  • HY-50880
    Elacridar hydrochloride

    GF120918A

    		 P-glycoprotein BCRP Cancer
    Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on drug distribution to brain and it can be used for the research of cancer.
  • HY-146096
    RMS3

    		P-glycoprotein Apoptosis Cancer
    RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property.
  • HY-N6932
    Voacamine

    		Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-N3085
    Phellamurin

    		P-glycoprotein Apoptosis Cancer Metabolic Disease
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
  • HY-U00247
    MCI826

    		P-glycoprotein Cancer
    MCI826 is a P-glycoprotein (P-gp) antagonist.
  • HY-19626
    NSC23925

    		P-glycoprotein Cancer
    NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.
  • HY-13646A
    Encequidar mesylate

    HM30181 mesylate; HM30181A mesylate

    		 P-glycoprotein Cancer
    Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
  • HY-13646
    Encequidar

    HM30181; HM30181A

    		 P-glycoprotein Metabolic Disease
    Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
  • HY-19642
    Glesatinib

    MGCD265

    		 TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    		 TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-107212
    Selamectin

    		Parasite Chloride Channel P-glycoprotein Bacterial Infection
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
  • HY-143792
    HTT-D3

    		P-glycoprotein Neurological Disease
    HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research.
  • HY-10550A
    Tariquidar methanesulfonate, hydrate

    XR9576 methanesulfonate, hydrate

    		 P-glycoprotein Cancer
    Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
  • HY-17384
    Valspodar

    PSC 833

    		 P-glycoprotein Cancer
    Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
  • HY-144366
    P-gp inhibitor 3

    		P-glycoprotein Cancer
    P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
  • HY-N0692
    Schisandrol B

    Gomisin-A; TJN-101; Wuweizi alcohol-B

    		 Reactive Oxygen Species Cytochrome P450 Autophagy Cancer
    Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities.
  • HY-146097
    RMS5

    		P-glycoprotein Apoptosis Cancer
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property.
  • HY-17013
    Dofequidar

    		P-glycoprotein Cancer
    Dofequidar(MS-209) is a novel quinoline compound, which can reverse P-glycoprotein (P-gp)-mediated MDR.
  • HY-146117
    P-gp modulator 2

    		P-glycoprotein Cancer
    P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
  • HY-146118
    P-gp modulator 3

    		P-glycoprotein Cancer
    P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
  • HY-125486
    Reversin 121

    		P-glycoprotein Cancer
    Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers.
  • HY-13574A
    Biricodar

    VX-710

    		 P-glycoprotein Cancer
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  • HY-110377
    Tariquidar dihydrochloride

    XR9576 dihydrochloride

    		 P-glycoprotein Cancer
    Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • HY-W009141
    1-Monopalmitin

    		P-glycoprotein Cancer
    1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells.
  • HY-10550
    Tariquidar

    XR9576

    		 P-glycoprotein Cancer
    Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • HY-100750
    Norverapamil hydrochloride

    (±)-Norverapamil hydrochloride; D591 hydrochloride

    		 Calcium Channel P-glycoprotein Drug Metabolite Cardiovascular Disease
    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.
  • HY-135328
    Norverapamil

    (±)-Norverapamil; D591

    		 Calcium Channel P-glycoprotein Drug Metabolite Cardiovascular Disease
    Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
  • HY-107643
    Reversan

    CBLC4H10

    		 P-glycoprotein Cancer
    Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
  • HY-112912
    P-gp modulator 1

    		P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-W001601
    Budipine

    		iGluR Neurological Disease
    Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease.
  • HY-121793
    Roemerine

    (-)-Roemerine

    		 P-glycoprotein Endogenous Metabolite Cancer
    Roemerine, an aporphine alkaloid, isolated from the leaves of Fibraurea recisa Pierre, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
  • HY-N0144
    Piperine

    Bioperine; 1-Piperoylpiperidine

    		 P-glycoprotein Autophagy Endogenous Metabolite Inflammation/Immunology Cancer
    Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.
  • HY-N0425
    Epoxylathyrol

    		P-glycoprotein Cancer
    Epoxylathyrol, an epoxylathyrane derivative isolated from the Euphorbia boetica, is a P-glycoprotein (P-gp) inhibitor. Epoxylathyrol is a P-gp-mediated multidrug resistance (MDR) reverser.
  • HY-N1941
    Isosinensetin

    		P-glycoprotein Bacterial Infection Inflammation/Immunology
    Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells.
  • HY-132866
    YS-370

    		P-glycoprotein Cancer
    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.
  • HY-N2103
    Tenacissoside G

    		P-glycoprotein Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-133948
    1-Monopalmitolein

    Glyceryl palmitoleate

    		 Others
    1-Palmitoleoyl glycerol is a biologically active monoacylglycerol. It increases daunomycin accumulation, shown to inhibit P-glycoprotein in Caco-2 cells. 1-Palmitoleoyl glycerol induces thymocyte apoptosis.
  • HY-N6684
    Deoxynivalenol

    		Others Metabolic Disease
    Deoxynivalenol, a mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors.
  • HY-135328S
    Norverapamil-d7

    (±)-Norverapamil-d7; D591-d7

    		 Calcium Channel P-glycoprotein Drug Metabolite Cardiovascular Disease
    Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
  • HY-135328AS
    Norverapamil-d7 hydrochloride

    (±)-Norverapamil-d7 (hydrochloride); D591-d7 (hydrochloride)

    		 Calcium Channel Cardiovascular Disease
    Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
  • HY-16191
    ELR510444

    		Microtubule/Tubulin Apoptosis Cancer
    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
  • HY-135336
    (R)-Verapamil hydrochloride

    (R)-(+)-Verapamil hydrochloride

    		 P-glycoprotein Apoptosis Cancer
    (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.
  • HY-15255
    Zosuquidar

    RS 33295-198; LY-335979

    		 P-glycoprotein Cancer
    Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.
  • HY-50671
    Zosuquidar trihydrochloride

    RS 33295-198 trihydrochloride; LY-335979 trihydrochloride

    		 P-glycoprotein Cancer
    Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.
  • HY-N10491
    Spongionellol A

    		P-glycoprotein Cancer
    Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer.
  • HY-N1916
    Coniferyl ferulate

    		Gutathione S-transferase P-glycoprotein Cancer
    Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST), reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM.
  • HY-N4108
    Hypophyllanthin

    		P-glycoprotein Cancer Inflammation/Immunology
    Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
  • HY-N10562
    Mutabilol

    		P-glycoprotein Cancer
    Mutabilol (compound 1) is a potent p-glycoprotein (P-gp) regulator. Mutabilol is a nature product could be isolated from Plectranthus mutabilis leaves. Mutabilol increases the P-gp expression in NCI-H460/R cells.
  • HY-113805
    MC70

    		P-glycoprotein Cancer
    MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC50 of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1.
  • HY-146391
    P-gp inhibitor 4

    		P-glycoprotein Cancer
    P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
  • HY-11018
    Risperidone

    R 64 766

    		 5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-N2947
    Boeravinone B

    		P-glycoprotein Infection Inflammation/Immunology
    Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress.
  • HY-14275
    Verapamil

    (±)-Verapamil; CP-16533-1

    		 Calcium Channel P-glycoprotein Cytochrome P450 Metabolic Disease
    Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
  • HY-A0064
    Verapamil hydrochloride

    (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride

    		 Calcium Channel P-glycoprotein Cytochrome P450 Cardiovascular Disease
    Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
  • HY-11018A
    Risperidone hydrochloride

    R 64 766 hydrochloride

    		 5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-126940
    Furanodiene

    		Reactive Oxygen Species P-glycoprotein Apoptosis Cancer
    Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level.
  • HY-135336S
    (R)-Verapamil-d7 hydrochloride

    (R)-(+)-Verapamil-d7 (hydrochloride)

    		 Isotope-Labeled Compounds P-glycoprotein Apoptosis Cancer
    (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[1][2].
  • HY-11018B
    Risperidone mesylate

    R 64 766 mesylate

    		 5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-N10492
    Spongionellol A analog 1

    		P-glycoprotein Cancer
    Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer.
  • HY-110232
    Risperidone-d4

    R 64 766-d4

    		 5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-N3028
    Taccalonolide B

    		Microtubule/Tubulin Cancer
    Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.
  • HY-A0064S
    Verapamil-d3 hydrochloride

    (±)-Verapamil-d3 (hydrochloride); CP-16533-1-d3 (hydrochloride)

    		 Calcium Channel P-glycoprotein Cytochrome P450 Cardiovascular Disease
    Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
  • HY-N0069
    Solamargine

    Solamargin; δ-Solanigrine

    		 P-glycoprotein Apoptosis Cancer
    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
  • HY-135194
    Risperidone E-oxime

    		Drug Metabolite Others
    Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
  • HY-132189
    Laniquidar

    R101933

    		 P-glycoprotein Cancer
    Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters. Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Laniquidar has limited oral bioavailability.
  • HY-A0064S2
    Verapamil-d3-1 hydrochloride

    (±)-Verapamil-d3-1 hydrochloride; CP-16533-1-d3-1 hydrochloride

    		 P-glycoprotein Calcium Channel Cytochrome P450
    Verapamil-d3-1 (hydrochloride) is the deuterium labeled Verapamil hydrochloride[1]. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[2][3][4].
  • HY-125374
    Larotaxel

    XRP9881

    		 Apoptosis Cancer
    Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
  • HY-17367A
    Atazanavir sulfate

    BMS-232632 sulfate

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Cancer Infection
    Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM.
  • HY-17367
    Atazanavir

    BMS-232632

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM.
  • HY-N2453
    Convallatoxin

    		PPAR NF-κB P-glycoprotein Cancer Inflammation/Immunology
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
  • HY-150565
    P-gp inhibitor 5

    		P-glycoprotein Cancer
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
  • HY-N2416
    Taccalonolide A

    		Microtubule/Tubulin Apoptosis Cancer
    Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
  • HY-17367S4
    Atazanavir-d6

    BMS-232632-d6

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
  • HY-15206
    Glibenclamide

    Glyburide

    		 Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
  • HY-17367S3
    Atazanavir-d5

    		HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
  • HY-17367S2
    Atazanavir-d9

    BMS-232632-d9

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
  • HY-15206S
    Glyburide-d11

    		Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
  • HY-15206S1
    Glyburide-d3

    Glyburide-d3

    		 Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
  • HY-101791
    P-gp inhibitor 1

    		P-glycoprotein Cancer
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  • HY-N10564
    8α,9α-Epoxycoleon-U-quinone

    		P-glycoprotein Cancer
    8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX.
  • HY-136589
    Verapamil EP Impurity C hydrochloride

    NSC-609249 hydrochloride

    		 Calcium Channel P-glycoprotein Cytochrome P450 Metabolic Disease
    NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
  • HY-12757
    YHO-13177

    		BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-15584A
    Taltobulin trifluoroacetate

    HTI-286 trifluoroacetate; SPA-110 trifluoroacetate

    		 Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-15584B
    Taltobulin hydrochloride

    HTI-286 hydrochloride; SPA-110 hydrochloride

    		 Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-15584
    Taltobulin

    HTI-286; SPA-110

    		 Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-14348
    GSK163090

    		5-HT Receptor Dopamine Receptor Neurological Disease
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities.
  • HY-151517
    SOS1-IN-14

    		Ras Cancer
    SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
  • HY-108511A
    PB28

    		Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-108511
    PB28 dihydrochloride

    		Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.
  • HY-B0387A
    Ibutilide

    U70226E free base

    		 Potassium Channel Cardiovascular Disease
    Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
  • HY-B0387
    Ibutilide fumarate

    U70226E

    		 Potassium Channel Cardiovascular Disease
    Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
  • HY-101453
    Ceefourin 1

    		Others Cancer
    Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
  • HY-119873
    Celiprolol

    REV 5320

    		 NO Synthase Adrenergic Receptor Cardiovascular Disease
    Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
  • HY-B1264
    Celiprolol hydrochloride

    		NO Synthase Adrenergic Receptor Cardiovascular Disease
    Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.