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Hydrocinchonine (Dihydrocinchonine) is a multidrugresistance (MDR)-reversal agent. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel in MES-SA/DX5 cells .
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrugresistance (MDR) and erythropoietic protoporphyria (EPP) .
Annamycin is an antibiotic, that has high affinity for lipid membranes and can bypass the multidrugresistance protein-1 (MDR-1 ) mechanism of cellular drug resistance. Annamycin exhibits antitumor efficacy in multilamellar vesicles against solid tumor .
Tolnapersine exhibits multidrugresistance (MDR) reversal activity, which reverses the resistance of tumor cells to multiple chemotherapy drugs by affecting P-glycoprotein (Pgp) on the cell membrane .
Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrugresistance(MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment .
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrugresistance. Reversin 121 can be used in the research of cancers .
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrugresistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrugresistance-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 .
Anti-inflammatory agent 57 (Compound 13), pyranocoumarin, is a nature product. Anti-inflammatory agent 57 can be isolated from the roots of Peucedanum praeruptorum. Anti-inflammatory agent 57 has multidrug-resistance (MDR) reversal and anti-inflammatory effect .
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 multidrugresistance (MDR) by selectively blocking the efflux function of ABCB1 .
Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrugresistance-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 .
Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrugresistance-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 .
PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrugresistance (MDR) reversal activity (IC50 = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression .
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrugresistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .
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 multidrugresistance (MDR) .
Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrugresistance-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 .
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 multidrugresistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .
Ganoderic acid R is a potent anticancer agent. Ganoderic acid R inhibits the growth by inducing apoptosis on tumor cell line. Ganoderic acid R possesses significant cytotoxicity on a multidrugresistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1) .
P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrugresistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells .
Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways .
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 multidrugresistance in cell lines overexpressing MDR-1 .
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrugresistance (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 .
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrugresistance. 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 .
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 multidrugresistance (MDR) reversal agent, shows a strong ability to reverse MDR .
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 multidrugresistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .
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 multidrugresistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrugresistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity .
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 multidrugresistance (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 .
P-gp modulator-7 (Compound 9e) is a P-glycoprotein (P-gp) inhibitor. P-gp modulator-7 occupies the channel entrance of P-gp with a unique T-shaped configuration, hindering the peristaltic extrusion mechanism of transmembrane domains TM12 and TM9, thereby inhibiting P-gp from pumping drugs out of cells and reversing the multidrugresistance (MDR) of tumor cells. P-gp modulator-7 is promising for research of cancers .
Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrugresistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrugresistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of 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 multidrugresistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrugresistance (MDR) cancers and can be used for cancer research.
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .
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-drugresistance (MDR) .
ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrugresistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity .
Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrugresistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and 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 multidrugresistance (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))
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrugresistance. Reversin 121 can be used in the research of cancers .
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrugresistance (MDR) cancers and can be used for cancer research.
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrugresistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
Hydrocinchonine (Dihydrocinchonine) is a multidrugresistance (MDR)-reversal agent. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel in MES-SA/DX5 cells .
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrugresistance (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 .
Anti-inflammatory agent 57 (Compound 13), pyranocoumarin, is a nature product. Anti-inflammatory agent 57 can be isolated from the roots of Peucedanum praeruptorum. Anti-inflammatory agent 57 has multidrug-resistance (MDR) reversal and anti-inflammatory effect .
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrugresistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .
Ganoderic acid R is a potent anticancer agent. Ganoderic acid R inhibits the growth by inducing apoptosis on tumor cell line. Ganoderic acid R possesses significant cytotoxicity on a multidrugresistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1) .
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 multidrugresistance (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 .
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrugresistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .
p-pg; PGP; ABCB1; MDR1; PGY1; multidrugresistance protein 1; ATP-binding cassette sub-family B member 1; P-glycoprotein 1; CD antigen CD243
WB
Human
P Glycoprotein Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 141 kDa, targeting to P Glycoprotein. It can be used for WB assays with tag free, in the background of Human.
ABC20; ABCB1; ATP binding cassette, sub family B(MDR/TAP), member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; multidrugresistance 1; multidrugresistance protein 1; P glycoprotein 1; P gp; PGY1.
IHC-P, IF-Tissue, IHC-F, WB
Human, Mouse, Rat
P Glycoprotein Antibody (YA6354) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein. It can be applicated for IHC-P, IF-Tissue, IHC-F, WB assays, in the background of human, mouse, rat.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; multidrugresistance 1; multidrugresistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, WB, ICC/IF, ELISA
Human, Mouse,
MDR1 Antibody (YA5626) is a mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to MDR1. It can be applicated for IHC-P, WB, ICC/IF, ELISA assays, in the background of human, mouse.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; multidrugresistance 1; multidrugresistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, ELISA
Human, Mouse,
MDR1 Antibody (YA5747) is a mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to MDR1. It can be applicated for IHC-P, ELISA assays, in the background of human, mouse.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; multidrugresistance 1; multidrugresistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
WB, IHC-P, ICC/IF, IP, ELISA
Human
MDR1 Antibody (YA6028) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to MDR1. It can be applicated for WB, IHC-P, ICC/IF, IP, ELISA assays, in the background of human.
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