Catalog No.
Product Name
Application
Product Information
Citations
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ORL1 Antagonist
ORL1 antagonist 2 is a selective antagonist of the opioid receptor-like 1 (ORL1). This compound has been primarily utilized in the study of P-glycoprotein (P-gp) interactions and transport mechanisms. Its ability to modulate ORL1 activity makes it a valuable tool in research aimed at understanding opioid signaling pathways and their implications in various physiological and pathological processes. -
Vitamin E
γ-Tocotrienol is an active form of vitamin E that primarily targets the signaling pathway of NF-κB and P-glycoprotein (P-gp). It demonstrates significant biological activity by reversing multidrug resistance (MDR) in breast cancer cells, enhancing the efficacy of chemotherapeutic agents. Additionally, γ-tocotrienol serves as a radioprotective agent, effectively mitigating bone marrow radiation damage associated with targeted radionuclide treatments. Research applications include cancer therapy and protection against radiation-induced injury. -
Antitumor Agent
Tyroservatide is a low-molecular-weight polypeptide recognized for its antitumor properties. It has demonstrated efficacy against hepatocellular carcinoma and lung cancer cells, making it a valuable tool for cancer research. Tyroservatide is utilized in studies aimed at elucidating its mechanisms of action and potential therapeutic applications in oncology. -
P-gp Inhibitor
P-gp Inhibitor 25 is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in drug transport and multidrug resistance. This compound enhances the oral bioavailability of paclitaxel, making it valuable in cancer therapy research. Its application in studies focused on overcoming P-gp-mediated drug resistance positions P-gp Inhibitor 25 as a significant tool in the development of effective anticancer treatments. -
P-gp Inhibitor
P-gp-IN-30 is a potent inhibitor of P-glycoprotein (P-gp) that acts by targeting Y-box binding protein 1 (YB-1). This compound enhances the sensitivity of cancer cells to Paclitaxel by decreasing both total and nuclear YB-1 protein levels, leading to the inhibition of P-gp expression and function, and consequently reducing the efflux of Paclitaxel. P-gp-IN-30 has demonstrated significant tumor growth inhibition in A549/Taxol xenograft mouse models and is applicable in research focused on non-small cell lung cancer (NSCLC). -
Histone Evictor
N,N-Dimethyl-idarubicin is a powerful histone evictor derived from idarubicin, functioning through a unique mechanism that avoids the induction of DNA double-strand breaks. This anthracycline compound exhibits effective cytotoxicity against Doxorubicin-resistant cells that overexpress the ABCB1 transporter. Its distinct action makes it valuable for research in cancer biology and therapeutic resistance studies. -
P-Glycoprotein Inhibitor
Reversin 205 is a selective inhibitor of P-glycoprotein (ABCB1), a crucial protein involved in drug transport and multidrug resistance. This compound serves as a peptide chemosensitizer, enhancing the efficacy of various chemotherapeutic agents by mitigating the efflux of drugs from cancer cells. Reversin 205 is applicable in research focused on overcoming drug resistance in cancer therapy and optimizing chemotherapy outcomes. -
P-glycoprotein Inhibitor
P-gp-IN-35 is a potent P-glycoprotein (P-gp) inhibitor, specifically designed to enhance the efficacy of chemotherapeutic agents. It demonstrates significant cytotoxic effects against breast and colorectal cancer cells, particularly in cases where P-gp is overexpressed, thus reversing multidrug resistance. This compound serves as a valuable tool in research focused on overcoming drug resistance in breast and colon cancers. -
P-glycoprotein Inhibitor
P-gp Inhibitor 5 is a selective inhibitor of P-glycoprotein (P-gp), a key player in multidrug resistance (MDR) in cancer. It exhibits notable antiproliferative activity against various cancer cell lines, effectively reinstating sensitivity to chemotherapeutic agents such as Vincristine and Paclitaxel in ABCB1/Flp-InTM-293 and KBvin cells. This property makes P-gp Inhibitor 5 a valuable tool for research aimed at overcoming drug resistance in cancer therapies. -
P-glycoprotein Inhibitor
KR30031 is a potent inhibitor of P-glycoprotein (P-gp), facilitating increased efficacy of anticancer drugs by overcoming multidrug resistance (MDR) pathways. This orally active compound is designed to enhance cytotoxic effects while minimizing cardiovascular side effects commonly associated with other P-gp inhibitors. KR30031 is valuable for research applications focused on understanding and reversing MDR in cancer therapeutic contexts. -
P-gp Inhibitor
P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that effectively reverses P-gp-mediated drug efflux. This 2,5-disubstituted furan derivative demonstrates significant affinity for P-gp through hydrogen bonding interactions with Asn 721 and Met 986. Its broad-spectrum reversal activity, coupled with low toxicity in MCF-7/ADR cell lines, makes P-gb-IN-1 a valuable tool for enhancing the efficacy of chemotherapeutic agents in research applications. -
Alkaloid
Coccinine is an alkaloid with a primary mechanism as a weak inhibitor of the serotonin transporter (SERT) and P-glycoprotein (P-gp), exhibiting IC50 values of 196.3 μM and 0.96 mM, respectively. This compound displays notable anti-tumor activity across various cancer cell lines, including MCF7, Hs578T, MDA-MB-231 (breast cancer), HCT-15 (colon cancer), and A549 (lung cancer). Coccinine serves as a valuable tool in the research of tumor biology and neurological disorders. -
P-glycoprotein MDR Modulator
XR9051 hydrochloride is a selective modulator of P-glycoprotein, acting specifically on its function to address multidrug resistance (MDR) in cancer cells. This compound enhances the efficacy of various chemotherapeutics by inhibiting the P-glycoprotein transport mechanism, thereby improving drug retention within resistant cell lines. XR9051 is utilized in research focused on overcoming drug resistance in oncology. -
P-glycoprotein Inhibitor
FM04 is a potent inhibitor of P-glycoprotein (P-gp) with an EC50 of 83 nM. It operates through two primary mechanisms: firstly, by binding to Q1193 and interacting with critical residues H1195 and T1226, and secondly, by engaging I1115, disrupting essential interactions within the R262-Q1081-Q1118 pocket, and uncoupling the ICL2-NBD2 interaction. FM04 is valuable for research exploring drug transport mechanisms and multidrug resistance in cancer therapies. -
P-gp Inhibitor
P-gp inhibitor 3 is a potent inhibitor of P-glycoprotein (P-gp), primarily targeting its ATPase activity to inhibit the efflux function. This compound demonstrates significant multidrug resistance (MDR) reversal capabilities, effectively enhancing the cytotoxic effects of antitumor agents such as Paclitaxel. P-gp inhibitor 3 is valuable in cancer research, particularly for studies focused on overcoming drug resistance in chemotherapy. -
P-gp Modulator
P-gp Modulator 2 is a potent competitive allosteric modulator of P-glycoprotein (P-gp). This compound significantly influences drug transport and can enhance the bioavailability of various therapeutic agents by inhibiting P-gp-mediated efflux. Its applications in research include studying drug-drug interactions and understanding mechanisms of multidrug resistance in cancer. -
P-gp Inhibitor
P-gp inhibitor 29 is a potent inhibitor of P-glycoprotein (P-gp) with an IC50 of 8.9 nM in Eca109/VCR cells. This compound not only inhibits P-gp activity but also induces apoptosis, making it a valuable tool in the study of drug resistance mechanisms in esophageal cancer. Its efficacy in modulating P-gp can facilitate research aimed at improving therapeutic strategies for this malignancy. -
P-gp Inhibitor
P-gp-IN-32 is a potent P-glycoprotein (P-gp) inhibitor that demonstrates significant ability to reverse multidrug resistance (MDR) in cancer cells. It exhibits low cytotoxicity with an IC50 of 0.11 μM and a reversal fold of 215.9 against Doxorubicin in MCF7/ADR cells. P-gp-IN-32 binds directly to P-gp, inducing conformational changes that inhibit its efflux function, making it a valuable tool for cancer research, particularly in studies focused on breast cancer. -
P-gp Inhibitor
P-gp Inhibitor 2 is a potent inhibitor of P-glycoprotein (P-gp), a critical transporter implicated in multidrug resistance. This compound effectively reverses Doxorubicin resistance with an IC50 of 0.22 µM in P-gp overexpressing human colorectal carcinoma SW600 Ad300 cells. Its application in cancer research highlights its potential as a valuable tool for overcoming P-gp-mediated drug efflux in therapeutic strategies. -
Pgp Inhibitor
P-gp inhibitor 15 is a nonsubstrate inhibitor targeting P-glycoprotein (P-gp), primarily acting to inhibit P-gp-ATPase activity. This compound effectively disrupts the P-gp-mediated efflux of Rhodamine123, leading to increased intracellular accumulation of chemotherapeutic agents. P-gp inhibitor 15 has demonstrated the ability to enhance the efficacy of Paclitaxel and shows potential in inhibiting tumor progression in xenograft models, specifically in nude mice with KBV tumors. -
P-glycoprotein Inhibitor
Dofequidar sesquifumarate is an orally active quinoline compound that functions as an inhibitor of P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). It exhibits a potent ability to reverse multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. This inhibition effectively blocks the efflux of chemotherapeutic agents, resulting in increased drug accumulation within cancer cells and enhanced chemotherapeutic efficacy. Dofequidar sesquifumarate is valuable for research applications aimed at overcoming drug resistance in cancer treatment. -
P-glycoprotein Inhibitor
(S)-Tenacissoside F is a polyoxypregnane compound that functions as a P-glycoprotein inhibitor. By effectively inhibiting the drug efflux activity of P-glycoprotein (P-gp/ABCB1), (S)-Tenacissoside F is capable of reversing multidrug resistance, making it a valuable compound in cancer research, particularly in the study of colon cancer. Its mechanism may provide insights into novel therapeutic approaches for overcoming drug resistance in tumors. -
P-gp Inhibitor
R 101933 is a potent inhibitor of P-glycoprotein (P-gp), a key mediator of drug efflux in cancer cells. By inhibiting P-gp, R 101933 enhances the intracellular accumulation of chemotherapeutic agents, making it valuable for studying drug resistance mechanisms in cancer research. This compound may also aid in identifying potential therapeutic strategies to improve the efficacy of anticancer drugs. -
P-gp Modulator
P-gp modulator 3 is a potent, competitive allosteric modulator of P-glycoprotein (P-gp). This compound enhances the effectiveness of therapeutic agents by inhibiting P-gp-mediated efflux, thus promoting improved intracellular accumulation of drugs. It is particularly useful in research applications focused on drug resistance mechanisms and the development of multi-drug resistance inhibitors. -
MDR Inhibitor
Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp), targeting multidrug resistance (MDR) in cancer cells. This compound demonstrates significant reversal activity against MDR both in vitro and in vivo, likely due to its ability to inhibit P-gp overexpression and enhance intracellular accumulation of anticancer agents. As a brominated derivative of tetrandrine, Bromotetrandrine is a valuable reagent for evaluating MDR modulation in tumor research. -
P-gp Modulator
P-gp inhibitor 4 is a selective modulator of P-glycoprotein, exhibiting an EC50 of 94 nM. This compound enhances the transport of therapeutic agents across the gastrointestinal barrier and can restore the efficacy of doxorubicin in multidrug-resistant cancer cells. It serves as a valuable tool for research into overcoming drug resistance and improving drug delivery mechanisms. -
P-gp Inhibitor
P-gp Inhibitor 26 is a potent inhibitor of P-glycoprotein (P-gp), a key player in multidrug resistance mechanisms. It effectively reverses P-gp-mediated drug resistance in K562/A02 cells, making it a valuable tool for investigating therapeutic strategies aimed at overcoming multidrug resistance in cancer cells. This compound is suitable for use in research applications focused on enhancing the efficacy of antitumor agents. -
P-gp Rransport Inhibitor
Phosphatidylinositol-1,2-dioctanoyl sodium acts as a potent inhibitor of P-glycoprotein (P-gp) transport. This compound demonstrates significant and reproducible inhibition of transmembrane P-gp transport, independent of cell line and substrate. Its involvement in signal transduction and cell motility makes it valuable for research into drug absorption and disposition, as well as studies on multidrug resistance in cancer therapy. -
P-gp Inhibitor
CJZ3 is a reversible inhibitor of P-glycoprotein (P-gp), which enhances the intracellular accumulation of the substrate drug Rh123. This compound is of particular interest in studies focused on improving drug permeability across the blood-brain barrier (BBB). CJZ3 has applications in research aimed at overcoming multidrug resistance and optimizing therapeutic efficacy for central nervous system-targeted therapies. -
P-glycoprotein Inhibitor
9,10-trans-Dehydroepothilone D is a potent P-glycoprotein inhibitor. It exhibits significant antiproliferative activity against paclitaxel-resistant cell lines that overexpress this transporter, making it a valuable tool in cancer research. Additionally, 9,10-trans-Dehydroepothilone D demonstrates tubulin polymerization activity, contributing to its potential use in elucidating mechanisms of drug resistance and improving therapeutic strategies. This compound serves as a promising candidate for further studies in cancer treatment paradigms. -
P-gp Inhibitor
Isotenulin acts as an inhibitor of P-glycoprotein (P-gp), enhancing the ATPase activity of P-gp and effectively combating multidrug resistance (MDR) in cancer cells. It demonstrates cytotoxic effects in both multidrug-resistant KB-vin cells and sensitive HeLaS3 cells. Additionally, Isotenulin shows a synergistic effect when used in conjunction with chemotherapeutic agents such as Paclitaxel, Vinblastine, and Doxorubicin, making it a valuable tool for research in cancer therapeutics. -
P-glycoprotein MDR Modulator
XR9051 is a specific modulator of P-glycoprotein, targeting multidrug resistance (MDR). This compound enhances the efficacy of chemotherapeutic agents by inhibiting P-glycoprotein activity, thereby improving drug accumulation in resistant cancer cells. XR9051 is primarily utilized in cancer research to investigate strategies for overcoming drug resistance and enhancing therapeutic outcomes. -
P-gp Inhibitor
8-Prenylchrysin is a C8-prenylated flavonoid that serves as a potent inhibitor of P-glycoprotein (P-gp). This compound demonstrates significant biological activity by modulating drug efflux, which can enhance the efficacy of chemotherapeutic agents. 8-Prenylchrysin is primarily utilized in cancer research to investigate its potential in overcoming multidrug resistance in tumor cells. -
P-glycoprotein Inhibitor
Encequidar hydrochloride is a potent P-glycoprotein (P-gp) inhibitor that enhances the oral bioavailability of P-gp substrate drugs. It exhibits exceptional potency with an IC50 of 0.63 nM, making it one of the most effective MDR1 inhibitors available. Encequidar significantly impedes the transepithelial transport of paclitaxel in MDCK monolayer cells, with an IC50 of 35.4 nM. This compound is valuable for research focused on pharmacokinetics and drug delivery systems. -
P-gp Inhibitor
Ardeemin, a P-glycoprotein inhibitor, effectively binds to and inhibits P-glycoprotein, thereby preventing the efflux of anticancer agents from cells. This mechanism helps to reverse the multidrug resistance phenotype in tumor cells, enhancing their sensitivity to chemotherapy. Ardeemin has demonstrated potential applications in cancer research, specifically in improving the efficacy of treatments for mammary carcinoma xenografts. -
Natural Compound
Jatrophane 5 is a natural compound derived from Jatropha carcas L., targeting P-glycoprotein (P-gp). It exhibits potent inhibitory activity against P-gp, surpassing that of R(+)-verapamil and Tariquidar in colorectal multi-drug resistant DLD1-TxR cells. This compound is valuable for research into overcoming multidrug resistance in cancer treatment and enhancing drug efficacy in resistant cell types. -
Thiosemicarbazone
NSC73306 is a thiosemicarbazone that acts as a cell-penetrating cytotoxic agent. It demonstrates heightened toxicity in cells that express functional P-glycoprotein (P-gp) compared to non-expressing cells. This compound is primarily utilized in research focused on drug resistance mechanisms and potential therapeutic strategies against multidrug-resistant cancers. -
M1 Positive Allosteric Modulator, P-gp Substrate
VU6007477 is a selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM, notable for its ability to penetrate the blood-brain barrier. This compound also acts as a human P-glycoprotein (P-gp) substrate and exhibits moderate permeability, providing advantages in central nervous system (CNS) research. As a pyranyl amide derivative, VU6007477 is a valuable tool for investigating cholinergic seizure activity and related neurological disorders. -
P-glycoprotein Inhibitor
MS-073 (CP162398) is a potent inhibitor of P-glycoprotein (P-gp), a key transporter involved in multidrug resistance. By competitively inhibiting the binding of chemotherapeutic agents to P-glycoprotein, MS-073 effectively reverses resistance in drug-resistant cancer cells. This compound is valuable for research into overcoming therapeutic challenges in oncology and drug delivery. -
P-glycoprotein Agonist
MCI826 is a P-glycoprotein (P-gp) agonist that enhances the efflux of various substrates across cell membranes. Its primary biological activity focuses on modulating drug transport and influencing cellular drug accumulation. This compound is valuable in research applications related to pharmacokinetics, multidrug resistance, and therapeutic strategies involving P-gp. -
Anti-parkinson Agent
Budipine is an anti-Parkinson agent that acts primarily as an N-methyl-D-aspartate (NMDA) antagonist while also influencing dopaminergic activity. It enhances dopamine release and inhibits monoamine oxidase type B (MAO-B), contributing to its therapeutic effects. As a substrate of P-glycoprotein (P-gp), Budipine's uptake into the brain is mediated by this transport mechanism. This compound is valuable for research into central nervous system disorders, including Parkinson's disease. -
Anti-parkinson Agent
Budipine hydrochloride functions primarily as an anti-Parkinson agent, targeting the central nervous system. It acts as a substrate of P-glycoprotein (P-gp), facilitating its uptake into the brain. Additionally, Budipine hydrochloride serves as an NMDA antagonist and exhibits indirect dopaminergic effects by enhancing dopamine release and inhibiting monoamine oxidase type B (MAO-B). This compound is valuable for research focused on CNS disorders, particularly Parkinson's disease. -
P-glycoprotein Inhibitor
NSC 23925B is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in multidrug resistance in cancer cells. This compound effectively reverses P-glycoprotein-mediated resistance and shows moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B is valuable for research focused on overcoming multidrug resistance in cancer therapy and studying P-glycoprotein's role in drug disposition. -
P-glycoprotein Inhibitor
Dofequidar fumarate is a potent P-glycoprotein (P-gp) inhibitor that also targets multidrug resistance-associated protein-1 (MDR-1). This quinoline compound effectively reverses multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. By blocking the efflux of chemotherapeutic agents, Dofequidar fumarate increases drug concentration within cancer cells, thereby enhancing the efficacy of chemotherapy. Its application is particularly relevant in cancer research focused on overcoming drug resistance. -
P-glycoprotein Inhibitor
Reversin 121 is a potent P-glycoprotein inhibitor that enhances the ATPase activity of the MDR1 gene product. By reversing P-glycoprotein-mediated multidrug resistance, it plays a critical role in overcoming drug resistance in cancer therapies. This compound is valuable for research applications focused on enhancing the efficacy of anticancer drugs in resistant cancer cell lines. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
P-Glycoprotein Inhibitor
Boeravinone B is a dual inhibitor of the NorA efflux pump in Staphylococcus aureus and human P-glycoprotein. This compound exhibits significant anti-biofilm activity and reduces intracellular bacterial invasion. Additionally, Boeravinone B demonstrates potential anti-aging and anti-apoptotic effects under oxidative stress conditions, making it a valuable reagent for research in microbiology and cellular aging pathways. -
P-glycoprotein Inhibitor
PGP-4008 is a selective inhibitor of P-glycoprotein (Pgp), known for its role in multidrug resistance (MDR) in cancer cells. This compound demonstrates significant antitumor activity by enhancing the efficacy of chemotherapeutic agents, particularly Doxorubicin, in murine models characterized by Pgp-mediated resistance. PGP-4008 is valuable for research into overcoming drug resistance in cancer therapy and the modulation of pharmacokinetics in oncology. -
P-glycoprotein
Hypophyllanthin is a significant lignan derived from Phyllanthus species that acts as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits strong anti-inflammatory properties and selectively inhibits P-gp activity without affecting multidrug resistance protein 2 (MRP2) activity. Its unique mechanism makes it a valuable tool for research in drug resistance and inflammation-related studies. -
P-glycoprotein Inhibitor
WS-898 is a potent P-glycoprotein inhibitor that effectively reverses paclitaxel resistance in various drug-resistant cancer cell lines, including SW620/Ad300, KB-C2, and HEK293/ABCB1, with IC50 values of 5.0, 3.67, and 3.68 nM, respectively. This compound serves as a valuable tool for research focused on overcoming multidrug resistance in cancer therapeutics. Its ability to inhibit ABCB1 transport activity makes it an important reagent for studies aimed at enhancing the efficacy of chemotherapeutic agents.
