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MDR reversers

" in MedChemExpress (MCE) Product Catalog:

By Targets:	P-glycoprotein (15) Reverse Transcriptase (1) Atg8/LC3 (1) Autophagy (1) BCRP (1) Cytochrome P450 (2) Endogenous Metabolite (2) FAK (1) Ferroptosis (1) HBV (1) HIV (1) NF-κB (2) p62 (1) PKA (1) PROTACs (1)
By Research Areas:	Cancer (15) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (1)

Inhibitors & Agonists

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Targets Recommended: Reverse Transcriptase P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101511

TTT-28	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 .

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-17013A

Dofequidar fumarate 2 Publications Verification MS-209	P-glycoprotein	Cancer
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-17013

Dofequidar 2 Publications Verification MS-209 free base	P-glycoprotein	Cancer
Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

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 .

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-106753

Tolnapersine	P-glycoprotein	Others
Tolnapersine exhibits multidrug resistance (MDR) reversal activity, which reverses the resistance of tumor cells to multiple chemotherapy drugs by affecting P-glycoprotein (Pgp) on the cell membrane .

HY-162396

P-gp inhibitor 21	P-glycoprotein	Cancer
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .

HY-17013D

Dofequidar sesquifumarate MS-209 sesquifumarate	P-glycoprotein	Cancer
Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-163981

ABCB1-IN-2	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 .

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 .

HY-N1457

Chrysosplenetin	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 .

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-161260

P-gp inhibitor 20	P-glycoprotein	Cancer
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC₅₀ value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .

HY-155152

P-gp/BCRP-IN-2	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 .

HY-108694R

γ-Tocotrienol (Standard)	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 .

HY-104012

Islatravir 2 Publications Verification MK-8591	HIV Reverse Transcriptase	Infection
Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC₅₀s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively. Islatravir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-W018791

Bifendate 1 Publications Verification 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) .

HY-163709

PROTAC FAK degrader 2	PROTACs FAK	Cancer
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC₅₀ of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC₅₀s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))

Cat. No.	Product Name	Target	Research Area

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-162396

P-gp inhibitor 21	P-glycoprotein	Cancer
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .

γ-Tocotrienol 1 Publications Verification	Structural Classification Monophenols Microorganisms other families Classification of Application Fields Source classification Phenols Plants Inflammation/Immunology Disease Research Fields	Endogenous Metabolite NF-κB
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 .

Chrysosplenetin	Flavonols Structural Classification Piscidia erythrina L. Flavonoids Classification of Application Fields Source classification Phenols Polyphenols Metabolic Disease Plants Compositae Disease Research Fields	P-glycoprotein Cytochrome P450 Ferroptosis
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 .

γ-Tocotrienol (Standard)	Structural Classification Monophenols Microorganisms other families Source classification Phenols Plants	Endogenous Metabolite NF-κB
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 .

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MDR reversers

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