Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
P-gp Inhibitor
YS-370 is a potent and selective inhibitor of P-glycoprotein (P-gp) that exhibits oral bioavailability. It facilitates the P-gp ATPase activity while demonstrating moderate inhibition of CYP3A4. This compound effectively reverses multidrug resistance (MDR) in cell lines such as SW620/AD300 and HEK293T-ABCB1, particularly in conjunction with paclitaxel, leading to enhanced antitumor efficacy. YS-370 is valuable for research focused on overcoming drug resistance in cancer therapy. -
P-gp Inhibitor
Tariquidar dihydrochloride is a potent and selective inhibitor of P-glycoprotein (P-gp), exhibiting a high affinity with a Kd of 5.1 nM. This compound significantly enhances the bioavailability of co-administered drugs by inhibiting P-gp-mediated drug efflux. It is widely used in research to investigate the roles of P-gp in pharmacokinetics, drug-drug interactions, and multidrug resistance in cancer therapies. -
P-gp Inhibitor
OY-101 is a potent and orally active inhibitor of P-glycoprotein (P-gp). This compound demonstrates the ability to sensitize drug-resistant tumors, effectively reversing multidrug resistance in cancer cells. With improvements in water solubility, cytotoxicity, and reversal activity compared to Tetrandrine, OY-101 represents a valuable tool in cancer research and development of therapeutic strategies for overcoming drug resistance. -
ABCB1 Inhibitor
Tariquidar dimesylate is a potent ABCB1 inhibitor targeting P-glycoprotein (P-gp). By binding to P-glycoprotein, it effectively increases the concentration of therapeutic agents within the brain, inhibiting their active transport out of cerebral tissue. This compound is invaluable for investigating blood-brain barrier permeability and understanding mechanisms of multidrug resistance in cancer and neurological research. -
P-glycoprotein Inhibitor
Encequidar mesylate hydrochloride is a selective inhibitor of P-glycoprotein (MDR1), which plays a crucial role in drug resistance. This compound enhances the anti-tumor efficacy of Paclitaxel in various mouse tumor models, making it valuable for cancer research. Encequidar mesylate hydrochloride is primarily utilized to study drug interactions and to evaluate therapeutic strategies aimed at overcoming multidrug resistance in cancer treatment. -
P-gp Inhibitor
P-gp Inhibitor 17 is a selective inhibitor of P-glycoprotein (P-gp), directly targeting its transmembrane domain to modulate its activity. This compound is particularly useful for investigating P-gp-mediated multidrug resistance in cancer cells, providing insights into therapeutic strategies for overcoming resistance in oncology research. Its role in enhancing drug bioavailability and efficacy makes it a valuable tool for studying tumor cell behavior and treatment response. -
P-gp Inhibitor
P-gp Inhibitor 13 specifically targets P-glycoprotein (P-gp), functioning as an inhibitor to reverse P-glycoprotein-mediated drug resistance. This compound has demonstrated effectiveness in overcoming paclitaxel resistance in A2780/T cells, making it a valuable tool in cancer research. Its applications extend to the study of advanced acute myeloid leukemia, providing insights into therapeutic strategies for overcoming resistance in this malignancy. -
P-glycoprotein Substrate
Neostenine is a stenine-type Stemona alkaloid that acts as a substrate for P-glycoprotein. It exhibits notable antitussive activity and demonstrates high absorptive permeability in Caco-2 monolayer models. Additionally, Neostenine shows oral bioactivity, making it relevant for research applications involving intestinal absorption and therapeutic potential in cough-related conditions. -
P-gp Inhibitor
P-gp inhibitor 14 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing P-gp-mediated multidrug resistance with an EC50 value of 48.74 nM. This compound demonstrates a weak inhibitory effect on CYP3A4 activity, making it a useful agent for enhancing the efficacy of chemotherapeutics in resistant cancer cells. Its primary applications include studies on drug transport mechanisms and overcoming resistance in multidrug-resistant tumors. -
P-gp Inhibitor
Clausarin is a selective P-glycoprotein (P-gp) inhibitor that effectively obstructs the P-gp-mediated efflux of chemotherapeutic agents. It demonstrates significant inhibition of daunorubicin efflux in K562/R7 human leukemia cells that overexpress P-gp, with Cyclosporin A serving as a positive control. Isolated from the roots of Citrus sinensis (sweet orange), Clausarin is a valuable reagent for research focused on overcoming multidrug resistance (MDR) in cancer therapies. -
P-gp/BCRP Inhibitor
P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models. -
Stable Isotope
Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems. -
L-type Calcium Channel Blocker
Norverapamil-d7 is a deuterium-labeled derivative of Norverapamil, which selectively targets L-type calcium channels. As an N-demethylated metabolite of Verapamil, it functions as an effective calcium channel blocker and inhibits P-glycoprotein (P-gp) activity. This reagent is suitable for research applications related to cardiovascular physiology, drug absorption studies, and pharmacokinetics involving P-gp transport mechanisms. -
Isotope-Labeled Compounds
Verapamil-d7 is a deuterium-labeled derivative of Verapamil, a calcium channel blocker and a potent inhibitor of the P-glycoprotein (P-gp) transporter. This isotope-labeled compound is utilized in pharmacokinetic studies and metabolic research, providing insights into drug interactions and transport mechanisms. Its applications extend to investigating conditions such as hypertension, cardiac arrhythmias, and angina, making it a valuable tool in cardiovascular research. -
Stable Isotope
Verapamil-d3 is a deuterium-labeled form of Verapamil, a calcium channel blocker that serves as a potent, orally active first-generation inhibitor of P-glycoprotein (P-gp) and CYP3A4. This stable isotope variant is utilized in pharmacokinetic studies and metabolic research, aiding in the investigation of cardiovascular diseases such as hypertension, arrhythmias, and angina. Verapamil-d3's unique properties make it an invaluable tool for studying drug interactions and bioavailability in various biological systems. -
Stable Isotope
Norverapamil-d6 hydrochloride is a stable isotope-labeled version of Norverapamil, an N-demethylated metabolite of Verapamil. This compound acts as a blocker of L-type calcium channels and inhibits P-glycoprotein (P-gp) function. It is primarily utilized in pharmacokinetic studies, drug metabolism research, and for tracing metabolic pathways in biological systems. -
L-type Calcium Channel Blocker
Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations. -
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. -
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.
