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MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity .
Hydrocinchonine (Dihydrocinchonine) is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .
Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (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 .
C2 Adamantanyl globotriaosylceramide (d18:1/2:0) (AdaGb3), a water-soluble globotriaosylceramide analog, is a bioactive sphingolipid. C2 Adamantanyl globotriaosylceramide (d18:1/2:0) reverses MDR1-MDCK cell drug resistance. C2 Adamantanyl globotriaosylceramide (d18:1/2:0) has high affinity for verotoxin (VT) .
AMPR-22 is an antimicrobial peptide. AMPR-22 can bind to the bacterial membrane and induces membrane permeabilization. AMPR-22 is effective against murine model of sepsis induced by MDR strains
PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrug resistance (MDR) reversal activity (IC50 = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression .
P-gp-IN-31 is a P-glycoprotein (P-gp) inhibitor with IC50 values of 0.42 μM for KB cells and 0.43 μM for MDR KBvin cells. P-gp-IN-31 can pass P-gp-mediated drug efflux mechanisms and shows collateral sensitivity via P-gp downregulation. P-gp-IN-31 inhibits cell proliferation, induces apoptosis and arrests the cell cycle at G2/M phase. P-gp-IN-31 can be used for the research of cancer, such as multidrug-resistant (MDR) malignancies .
Sulbactam (Standard) is the analytical standard of Sulbactam. This product is intended for research and analytical applications. Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
Sulbactam (sodium) (Standard) is the analytical standard of Sulbactam (sodium). This product is intended for research and analytical applications. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
PA3552-IN-1 (compound 15) is an antibiotic adjuvant that restores sensitivity of MDRP. aeruginosa DK2 strain to Polymyxin B. PA3552-IN-1 can reduce PA3552 expression .
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 multidrug resistance (MDR) of tumor cells. P-gp modulator-7 is promising for research of cancers .
MDP1, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
MDP1 acetate, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 acetate has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
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 .
Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity .
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistant K. pneumoniae. K11 has high thermal and wide pH stability .
IITR01324 is an antimicrobial agent. IITR01324 has antimicrobial activity against Escherichia coli (MIC = 3.58 mg/L) and other Gram-negative bacteria (Shigella flexneri: MIC = 3.58 mg/L; Cronobacter sakazakii: MIC = 28.63 mg/L). IITR01324 exerts its antimicrobial activity by destroying bacterial DNA after activation of intracellular reductases. IITR01324 can be used to study the development of new antimicrobial drugs, especially against multidrug-resistant (MDR) pathogens .
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely .
SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity .
P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
Limonianin (Atalantoflavone) is a flavone, that can be isolated from Erythrina sigmoidea and the root bark of Citrus limonia. Limonianin presents inhibitory effect against P. gingivalis. Limonianin shows cytotoxic activity against multidrug-resistant (MDR) cancer cell lines .
MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers .
IITR01324 (Standard) is the analytical standard of IITR01324. This product is intended for research and analytical applications. IITR01324 is an antimicrobial agent. IITR01324 has antimicrobial activity against Escherichia coli (MIC=3.58 mg/L) and other Gram-negative bacteria (Shigella flexneri: MIC=3.58 mg/L; Cronobacter sakazakii: MIC=28.63 mg/L). IITR01324 exerts its antimicrobial activity by destroying bacterial DNA after activation of intracellular reductases. IITR01324 can be used to study the development of new antimicrobial drugs, especially against multidrug-resistant (MDR) pathogens .
(R)-DS86760016 is the R-enantiomer of DS86760016 (HY-124679). DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa .
Benzyldodecyldimethylammonium chloride dihydrate is a quaternary ammonium compound (QAC) and can be used as a biocide to target antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant (MDR) P. aeruginosa et. al. Benzyldodecyldimethylammonium chloride dihydrate, an antimicrobial agent, bacteriostatic or bactericidal properties depending on the concentration.
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 .
DprE1-IN-9 (compound B18) is an effective reversible DprE1 inhibitor and can bind to the receptor cavity of DprE1. DprE1-IN-9 shows strong antimycobacterial activity not only against non-pathogenic strain H37Ra (MIC=0.18 µg/mL) but also against pathogenic H37Rv and the clinical MDR and XDR isolates .
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 .
Antibacterial agent 287 (Compound 26), a derivative of Deoxynybomycin (HY-116926), is an antibacterial agent. Antibacterial agent 287 has potent antibacterial activity against a variety of Gram-negative bacterium with MICs of 0.5, 0.5 and 0.06 μg/mL for WT S. aureus, WT E. coli and E. coli ΔtolC, respectively. Antibacterial agent 287 can be used for multidrug-resistant (MDR) bacterium infections research .
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 .
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 .
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 multidrug resistance (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 .
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
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 .
Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
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 (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) .
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 multidrug resistance (MDR) cancers and can be used for cancer research.
BAL-30072, a siderophore sulfactam, is a monocyclic beta-lactam antibiotic, with activity against multiresistant gram-negative bacilli. BAL30072 shows MIC90 values of 4 μg/mL for MDRAcinetobacter spp. and 8 μg/mL for MDRP. aeruginosa, respectively .
P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
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) .
Fosfomycin (calcium) (Standard) is the analytical standard of Fosfomycin (calcium). This product is intended for research and analytical applications. Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
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 .
Telomycin is a calcium-dependent antibiotic, which can be produced by Streptomyces. Telomycin inhibits gram-positive bacteria, including multidrug-resistant (MDR) pathogens .
Cinerubin R has anti-Gram-positive bacteria and inhibition of tumor cell activity, and its inhibition effect on multidrug resistant (MDR) cells is the same as that on protocells .
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc .
Ardeemin ((-)-Ardeemin) binds to the P-glycoprotein, preventing anticancer agent from being pumped out of cells. Ardeemin reverses the multidrug resistance phenotype of tumor cells and increases the sensitivity of tumor cells to anticancer agent in mammary carcinoma xenografts .
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 .
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 .
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 .
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+ .
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 .
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 .
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 .
Hydrocinchonine (Dihydrocinchonine) (Standard) is the analytical standard of Hydrocinchonine (HY-W035709). This product is used for research and analytical purposes.Hydrocinchonine is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .
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 .
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 .
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains .
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 .
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 .
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 .
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 .
Antimalarial agent 44 (Compound 3) is an antimalarial agent against parasite. Antimalarial agent 44 has a good permeability across MDCK-MDR1 cell monolayers and a high clearance by mouse liver microsomes .
Mtb-IN-8 (compound 5jb) is an orally active inhibitor of Mycobacterium tuberculosis (Mtb) with MIC values of 0.03 μg/mL for H37Rv and 0.125-0.06 μg/mL for MDR-Mtb, respectively .
DprE1-IN-11 (compound 3) is an orally active DprE1 inhibitor with antituberculosis activity against MTB H37Rv and MDR-MTB strains (MIC <0.029-0.095 μM) .
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 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 .
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 .
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 multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) .
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin .
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 .
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 .
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice .
Lynronne-3 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-128 μg/mL for methicillin-resistant MRSA strains). Lynronne-3 is also effective against P. aeruginosa infection
Antitubercular agent-13 (Compound 3d) is an antitubercular agent with MIC values of 0.007 µg/mL and 1.851 µg/mL against MTB H37Rv and MDR-MTB 16833, respectively. Antitubercular agent-13 shows metabolic instability .
MTC420 (compound 42a) is a heterocyclic quinolone compound that targets the respiratory chain of Mycobacterium tuberculosis and exhibits antituberculosis activity (Rep Mtb: IC50=525 nM, Wayne Mtb: IC50=76 nM, MDR Mtb: IC50=140 nM) .
Lynronne-2 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-256 μg/mL for methicillin-resistant MRSA strains). Lynronne-2 is also effective against P. aeruginosa infection
Antibacterial agent 240 (compound 62-7c) is an antibacterial agent that can target multidrug-resistant (MDR) MRSA strains. Antibacterial agent 240 showed high biosafety and potent anti-infection activity in mouse pneumonia and mouse wound models of MRSA infection .
Bisantrene (Standard) is the analytical standard of Bisantrene. This product is intended for research and analytical applications. 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 .
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
Tampramine (47), a phenothiazine, could reverse multidrug resistance, with ED50 values of 60 μM (P388 cells) and 60 μM (P388/ADR cells), respectively .
Isoquinoline is an analog of pyridine. Isoquinoline-based alkaloids, such as p-tolyl bisisoquinoline, phthaloyl isoquinoline, and naphthyl isoquinoline, exhibit anticancer activity.
Berberine, an isoquinoline alkaloid, exerts anti-inflammatory effects in diabetic mice by downregulating the gene expression ratios of pro-/anti-inflammatory and Th1/Th2 cytokines.
Additionally, some isoquinoline-based compounds also possess antidepressant, antibacterial, antimalarial, and anti-HIV activities .
ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity .
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
WCK-5153 is a Penicillin-Binding Protein 2 (PBP2) inhibitor with an IC50 of 0.14 μg/ml (for P. aeruginosa PBP2) and acts as a β-lactam enhancer against Pseudomonas aeruginosa. WCK-5153 can be used in studies of multidrug-resistant (MDR) pathogens .
BWC0977 is a potent bacterial topoisomerase inhibitor that inhibits bacterial DNA replication via inhibition of DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) of 0.03-2 µg/mL against MDR (Multi-Drug Resistant) Gram-negative bacteria .
(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) (Compound 4a) is a Gram-negative outer membrane permeabilizer with synergistic antibacterial activity through the blockage on LptA/LptC interaction via targeting Met47 in LptA. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) potentiates pol B against both wild-typed and MDR A. baumannii and E. coli strains. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) can be used as antibiotic adjuvants against MDR Gram-negative bacteria .
Antibacterial agent 216 (Compound 2a) is an antibacterial agent that exhibits significant bactericidal effects when combined with INH and RIF. Antibacterial agent 216 has demonstrated remarkable in vitro anti-tuberculosis activity against Mtb H37Rv and MDR clinical isolates and can be used for tuberculosis research .
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) .
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 .
KR30031, a Verapamil (HY-14275) analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting P-gp with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer .
N-Deacetylthiocolchicine is a tubulin inhibitor with an IC50 value of 2.2 nM in MDR-negative MDA-MB 231 breast cancer cells. N-Deacetylthiocolchicine exerts antiproliferative activity by binding to tubulin to interfere with microtubule assembly, arresting cells in mitosis during the cell cycle. N-Deacetylthiocolchicine is promising for research of malignancies such as breast 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 .
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 multidrug resistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1) .
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice .
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 multidrug resistance (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 .
RCB18350 is an antituberculosis agent that belongs to the class of isoxazole derivatives. RCB18350 has bacteriostatic activity and inhibits the growth of Mycobacterium tuberculosis with an MIC of 1.25 μg/mL. RCB18350 is effective against multidrug-resistant Mycobacterium tuberculosis (MDR-TB) clinical isolates, slow-growing mycobacteria such as Mycobacterium bovis BCG and Mycobacterium avium .
Methyl oleate is a fatty acid methyl ester (FAME) with anti-extended spectrum β-Lactamase (ESBL) potential, anticancer and antibacterial activities. Methyl oleate substantially improves the antioxidation ability but markedly impaired the antiwear capacity of zinc dialkyldithiophosphate (ZDDP). Methyl oleate is promising for research of ESBL producing multi drug resistant (MDR) pathogens .
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 .
Lynronne-1 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including MDR strains (MIC: 8-32 μg/mL for methicillin-resistant MRSA strains). Lynronne-1 reduces the bacterial load in MRSA infected wound murine model. Lynronne-1 is also effective against P. aeruginosa infection .
SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L .
DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC50s of 0.38, 0.62, and 0.16 μM, respectively .
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 .
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 .
Fudapirine, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. Fudapirine exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. Fudapirine also inhibits hERG channel with the IC50 of 1.89 μM.
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (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) .
BMS-986020 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist . BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively . BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) .
BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist . BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively . BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) .
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 . 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 .
CYP1A1-IN-1 (Compound 47) is a small-molecule cytochrome P4501A1 (CYP1A1) inhibitor. CYP1A1-IN-1 reduces the bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii by enhancing macrophage phagocytosis. CYP1A1-IN-1 is promising for research of sepsis caused by multidrug-resistant (MDR) bacteria .
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
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) .
XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
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 multidrug resistance (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 .
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.
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 .
Anti-MRSA agent 28 is an antibacterial agent against multidrug resistant (MDR) gram-positive strains with MICs of 0.06-0.125 μg/mL. Anti-MRSA agent 28 can target DNA polymerase IIIC to reduce the amount of genomic DNA with the IC50 of 3.80 μg/mL. Anti-MRSA agent 28 has good antibacterial activity and reduces inflammation. Anti-MRSA agent 28 can be used against gram-positive strains and infectious conditions.
Anti-MRSA agent 26 is a potent anti-MRSA agent with MIC <0.015 μg/mL. Anti-MRSA agent 26 has superior activity against a broad range of Gram-positive pathogens and shows no cytotoxicity in three mammalian cell lines (Caco-2, DU-145 and MDCKII MDR1 cells) at 10 μM. Anti-MRSA agent 26 has a robust TAP pharmacophore and an excellent antibacterial activity in Staphylococcus aureus skin infection mice model .
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 multidrug resistance (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 multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .
Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-agent resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages . Antibacterial agent 106 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Xeruborbactam disodium is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam disodium inhibits key serine and metallo beta-lactamases at a nano molar range .
PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection .
Xeruborbactam is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam inhibits key serine and metallo beta-lactamases at a nano molar range .
Mtb-IN-10 (Compound P15) is a Rv1625c/Cya activator that regulates cAMP metabolism to influence the growth of Mycobacterium tuberculosis (Mtb). Mtb-IN-10 exhibits an EC50 of 1.96 µM in an Mtb-infected macrophage model and demonstrates 58.0% oral bioavailability in mice at a 20 mg/kg dose. It may regulate intracellular signaling and disrupt cholesterol metabolism in Mtb, thereby inhibiting bacterial proliferation. Mtb-IN-10 holds potential for tuberculosis (TB) research, particularly for combating multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) Mtb strains .
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 multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer .
PA2-GNU7 is an antimicrobial peptide (AMP). PA2-GNU7 exhibits potent antimicrobial activity with minimal inhibitory concentration (MIC) against P. aeruginosa, E. coli, S. typhimurium, S. aureus, and C. albicans are 2 μM, 1 μM, 2 μM, 2 μM, and 8 μM, respectively. PA2-GNU7 rapidly and selectively kills Pseudomonas aeruginosa without affecting other commensal bacteria. PA2-GNU7 significantly improves survival of mice infected with P. aeruginosa. PA2-GNU7 can be used for the research and development of therapeutic agents against MDRPseudomonas aeruginosa infections .
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))
Pulchinenoside C (Standard) is the analytical standard of Pulchinenoside C. This product is intended for research and analytical applications. Pulchinenoside C (Anemoside B4) is a natural compound of the herbaceous peony saponin B4, which has many biological effects, such as antitumor, neuroprotective, and anti-angiogenic activities.
MDP1 acetate, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 acetate has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistant K. pneumoniae. K11 has high thermal and wide pH stability .
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 .
AMPR-22 is an antimicrobial peptide. AMPR-22 can bind to the bacterial membrane and induces membrane permeabilization. AMPR-22 is effective against murine model of sepsis induced by MDR strains
MDP1, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
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 multidrug resistance (MDR) cancers and can be used for cancer research.
Telomycin is a calcium-dependent antibiotic, which can be produced by Streptomyces. Telomycin inhibits gram-positive bacteria, including multidrug-resistant (MDR) pathogens .
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 .
Lynronne-3 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-128 μg/mL for methicillin-resistant MRSA strains). Lynronne-3 is also effective against P. aeruginosa infection
Lynronne-2 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-256 μg/mL for methicillin-resistant MRSA strains). Lynronne-2 is also effective against P. aeruginosa infection
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
Lynronne-1 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including MDR strains (MIC: 8-32 μg/mL for methicillin-resistant MRSA strains). Lynronne-1 reduces the bacterial load in MRSA infected wound murine model. Lynronne-1 is also effective against P. aeruginosa infection .
PA2-GNU7 is an antimicrobial peptide (AMP). PA2-GNU7 exhibits potent antimicrobial activity with minimal inhibitory concentration (MIC) against P. aeruginosa, E. coli, S. typhimurium, S. aureus, and C. albicans are 2 μM, 1 μM, 2 μM, 2 μM, and 8 μM, respectively. PA2-GNU7 rapidly and selectively kills Pseudomonas aeruginosa without affecting other commensal bacteria. PA2-GNU7 significantly improves survival of mice infected with P. aeruginosa. PA2-GNU7 can be used for the research and development of therapeutic agents against MDRPseudomonas aeruginosa infections .
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
Hydrocinchonine (Dihydrocinchonine) is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .
Limonianin (Atalantoflavone) is a flavone, that can be isolated from Erythrina sigmoidea and the root bark of Citrus limonia. Limonianin presents inhibitory effect against P. gingivalis. Limonianin shows cytotoxic activity against multidrug-resistant (MDR) cancer cell lines .
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 .
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc .
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 .
Cinerubin R has anti-Gram-positive bacteria and inhibition of tumor cell activity, and its inhibition effect on multidrug resistant (MDR) cells is the same as that on protocells .
Ardeemin ((-)-Ardeemin) binds to the P-glycoprotein, preventing anticancer agent from being pumped out of cells. Ardeemin reverses the multidrug resistance phenotype of tumor cells and increases the sensitivity of tumor cells to anticancer agent in mammary carcinoma xenografts .
Hydrocinchonine (Dihydrocinchonine) (Standard) is the analytical standard of Hydrocinchonine (HY-W035709). This product is used for research and analytical purposes.Hydrocinchonine is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains .
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 .
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 .
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice .
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 .
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 multidrug resistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1) .
Methyl oleate is a fatty acid methyl ester (FAME) with anti-extended spectrum β-Lactamase (ESBL) potential, anticancer and antibacterial activities. Methyl oleate substantially improves the antioxidation ability but markedly impaired the antiwear capacity of zinc dialkyldithiophosphate (ZDDP). Methyl oleate is promising for research of ESBL producing multi drug resistant (MDR) pathogens .
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 .
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (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) .
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 . 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 .
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 multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .
Pulchinenoside C (Standard) is the analytical standard of Pulchinenoside C. This product is intended for research and analytical applications. Pulchinenoside C (Anemoside B4) is a natural compound of the herbaceous peony saponin B4, which has many biological effects, such as antitumor, neuroprotective, and anti-angiogenic activities.
CXCR5/CD185 Protein-VLP, Human (HEK293) is the recombinant human-derived CXCR5/CD185 protein, expressed by HEK293, with C-His tag.Formed in HEK293 cultures, these VLPs concentrate membrane proteins on the cell surface, producing high-concentration proteins ideal for immunization and antibody screening. Given the high immunogenicity of VLPs, the immunization protocol such as antigen dose, schedule, and adjuvant, requires optimization. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P705433. Tags can only be detected under denaturing conditions.
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
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; Multidrug resistance 1; Multidrug resistance 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.
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; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, WB, ICC/IF, ELISA
Human, Mouse,
P Glycoprotein Antibody (YA5626) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
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; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, ELISA
Human, Mouse,
P Glycoprotein Antibody (YA5747) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
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; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
WB, IHC-P, ICC/IF, IP, ELISA
Human
P Glycoprotein Antibody (YA6028) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein.
CYP1A1-IN-1 (Compound 47) is a small-molecule cytochrome P4501A1 (CYP1A1) inhibitor. CYP1A1-IN-1 reduces the bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii by enhancing macrophage phagocytosis. CYP1A1-IN-1 is promising for research of sepsis caused by multidrug-resistant (MDR) bacteria .
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