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Results for "

MDR1

" in MedChemExpress (MCE) Product Catalog:

29

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

7

Natural
Products

2

Recombinant Proteins

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108347
    CP-100356 hydrochloride
    4 Publications Verification

    P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) [1].
    CP-100356 hydrochloride
  • HY-125486

    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 [1] .
    Reversin 121
  • HY-100875
    Bisantrene
    5 Publications Verification

    CL216942

    Topoisomerase Cancer
    Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1 [1] .
    Bisantrene
  • HY-100875A
    Bisantrene dihydrochloride
    5 Publications Verification

    CL-216942 dihydrochloride

    Topoisomerase Cancer
    Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1 [1] .
    Bisantrene dihydrochloride
  • HY-N1941

    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 [1] .
    Isosinensetin
  • HY-N6789
    KT5720
    3 Publications Verification

    PKA Neurological Disease Cancer
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases [1] .
    KT5720
  • HY-13554

    Antibiotic Infection Cancer
    Annamycin is an antibiotic, that has high affinity for lipid membranes and can bypass the multidrug resistance protein-1 (MDR-1 ) mechanism of cellular drug resistance. Annamycin exhibits antitumor efficacy in multilamellar vesicles against solid tumor [1].
    Annamycin
  • HY-13646C

    HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride

    P-glycoprotein Cancer
    Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models [1] .
    Encequidar mesylate hydrochloride
  • HY-N10491

    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 [1].
    Spongionellol A
  • HY-N10492

    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 [1].
    Spongionellol A analog 1
  • HY-161353

    c-Met/HGFR P-glycoprotein Cancer
    c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC50 = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent [1].
    c-Met-IN-23
  • HY-101511

    P-glycoprotein Cancer
    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 [1].
    TTT-28
  • HY-N1457

    P-glycoprotein Cytochrome P450 Ferroptosis Metabolic Disease
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A [1].
    Chrysosplenetin
  • HY-13646B

    HM30181 hydrochloride; HM30181A hydrochloride

    P-glycoprotein Others
    Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM [1].
    Encequidar hydrochloride
  • HY-156088

    Microtubule/Tubulin Apoptosis Cancer
    SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 [1].
    SSE1806
  • HY-N6022

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects [1]. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of agent-agent interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones .
    Byakangelicin
  • HY-155152

    P-glycoprotein BCRP Cancer
    P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells [1].
    P-gp/BCRP-IN-2
  • HY-B0766

    SY801

    Autophagy Apoptosis HBV HCV HSP Reactive Oxygen Species Bcl-2 Family Glutathione S-transferase p38 MAPK NF-κB Microtubule/Tubulin ERK JNK TNF Receptor Interleukin Related CDK Cyclin G-associated Kinase (GAK) mTOR P-glycoprotein Ferroptosis Infection Inflammation/Immunology Cancer
    Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma [1] .
    Bicyclol
  • HY-13776A

    P-glycoprotein Cancer
    XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR) .
    XR9051 hydrochloride
  • HY-13776

    P-glycoprotein Cancer
    XR9051 is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR) .
    XR9051
  • HY-17013D

    MS-209 sesquifumarate

    P-glycoprotein Cancer
    Dofequidar sesquifumarate (MS-209) is a novel quinoline compound, which can reverse P-glycoprotein (P-gp)-mediated MDR .
    Dofequidar sesquifumarate
  • HY-112912

    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) .
    P-gp modulator 1
  • HY-162068

    Others Cancer
    Auristatin23, a conjugate of Auristatin F (HY-15583), is a cytotoxin. Auristatin23 exhibit cytotoxic activities towards targeted cells, including abnormal cells such as cancer cells, that are MDR+ .
    Auristatin23
  • HY-10982A

    AS1413 dihydrochloride

    Others Others
    Amonafide dihydrochloride (AS1413 dihydrochloride) is a topoisomerase II (Topo II) inhibitor and DNA intercalator with activity in inducing apoptotic signaling. Amonafide dihydrochloride can inhibit the binding of Topo II to DNA, thereby preventing the synthesis of DNA and RNA. Amonafide dihydrochloride maintains cytotoxic activity in the presence of P-glycoprotein-mediated multidrug resistance (MDR) .
    Amonafide dihydrochloride
  • HY-108694
    γ-Tocotrienol
    1 Publications Verification

    Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment [1] .
    γ-Tocotrienol
  • HY-108694R

    Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment [1] .
    γ-Tocotrienol (Standard)
  • HY-W018791

    DDB

    HBV Autophagy Cytochrome P450 Atg8/LC3 p62 P-glycoprotein Infection Cardiovascular Disease Cancer
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR) .
    Bifendate
  • HY-163981

    P-glycoprotein Cancer
    ABCB1-IN-2 (compound 16q) is a functional inhibitor that can directly bind to the ABCB1 protein and stabilize its structure without affecting the expression and subcellular localization of ABCB1. ABCB1-IN-2 can increase the sensitivity of MCF-7/ADR cells to paclitaxel (PTX), increase the accumulation of PTX, and prevent the accumulation and excretion of luciferin Rh123 mediated by ABCB1. ABCB1-IN-2, as an ABCB1-mediated multidrug resistance (MDR) reversal agent, shows a strong ability to reverse MDR .
    ABCB1-IN-2
  • HY-149936

    HIV Protease Infection
    HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1 (HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant [1].
    HIV-1 protease-IN-8

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