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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Kv1.5 Inhibitor
MK-1832 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 86 nM. As a P-glycoprotein substrate, MK-1832 is particularly relevant for studying atrial fibrillation and related cardiovascular disorders. Its specificity for Kv1.5 makes it a valuable tool for investigating the molecular mechanisms underlying cardiac arrhythmias and for evaluating potential therapeutic interventions. -
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-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. -
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. -
KV1.3 Inhibitor
KV1.3-IN-2 hydrochloride is a selective inhibitor of the KV1.3 potassium channel, with no impact on hERG channel activity. This compound is particularly valuable in the study of immune-related diseases, including psoriasis, rheumatoid arthritis, and systemic lupus erythematosus, due to its ability to modulate KV1.3-mediated cellular processes. Researchers can utilize KV1.3-IN-2 hydrochloride to explore mechanisms underlying these conditions and develop potential therapeutic strategies. -
Nav1.7 Inhibitor
Nav1.7-IN-19 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.49 μM. This compound exhibits significant selectivity for Nav1.7, with 312-fold and 662-fold selectivity over Nav1.1 and Nav1.5 in their inactivated states, respectively. Additionally, Nav1.7-IN-19 shows minimal inhibition of hERG potassium channels. Due to its analgesic properties, Nav1.7-IN-19 is valuable for research focused on neurological diseases. -
CPS1 Inhibitor
H3B-120 is a selective inhibitor of carbamoyl phosphate synthetase 1 (CPS1) that functions through competitive allosteric modulation, exhibiting an IC50 of 1.5 μM and a Ki of 1.4 μM. This compound demonstrates anti-cancer activity, making it a valuable tool for research into metabolic and oncological pathways. H3B-120 can be utilized in studies investigating the role of CPS1 in cancer metabolism and therapeutic targeting. -
Complex II Inhibitor
Atpenin A5 is a highly selective inhibitor of complex II, with an IC50 of approximately 10 nM. This compound acts as a potent mKATP channel agonist, offering cardioprotective effects. It is valuable for research applications focused on mitochondrial function, cardiac physiology, and energy metabolism. -
Kir6.2 Inhibitor
L-Palmitoylcarnitine chloride is a selective inhibitor of the Kir6.2 subunit of KATP channels. It disrupts membrane lipid homeostasis during ischemic conditions by accumulating in the sarcolemma while inhibiting channel activity without altering single-channel conductance. This compound is valuable for research into metabolic disturbances and the role of KATP channels in cardiac and skeletal muscle physiology. -
SK Channels Inhibitor
NS8593 hydrochloride is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels). This compound demonstrates reversible inhibition of SK3-mediated currents with a Kd value of 77 nM, as well as inhibiting SK1-3 subtypes in a Ca2+-dependent manner (Kds of 0.42, 0.60, and 0.73 μM respectively at 0.5 μM Ca2+). Importantly, NS8593 hydrochloride does not affect intermediate and large conductance Ca2+-activated K+ channels, such as hIK and hBK channels. It is valuable for research applications exploring the role of SK channels in cellular signaling and excitability. -
TMEM175 Inhibitor
AP-6 is a selective inhibitor of TMEM175, targeting lysosomal function modulation. This compound enhances lysosomal macromolecular catabolism, promoting accelerated digestive processes in macrophages and other cell types. AP-6 is a valuable tool in research related to Parkinson's disease, providing insights into lysosomal dysregulation and its implications in neurodegeneration. -
Ca2+-activated K+ Channel Inhibitor
Iberiotoxin is a potent inhibitor of Ca2+-activated K+ channels, derived from the venom of the Buthus tamulus scorpion. It demonstrates high specificity and selectivity, with an affinity (Kd) of approximately 1 nM, effectively blocking high conductance channels without affecting other voltage-dependent ion channels. This characteristic makes Iberiotoxin a valuable tool for investigating the physiological roles of Ca2+-activated K+ channels in various biological processes and for exploring their relevance in neurophysiological and cardiological research applications. -
Kv12.2 (KCNH3) Inhibitor
ASP2905 is a potent inhibitor of the potassium channel Kv12.2 (KCNH3), encoded by the Kcnh3/BEC1 gene. This compound is orally active and capable of crossing the blood-brain barrier, exhibiting significant antipsychotic properties. ASP2905 is valuable for studying the roles of Kv12.2 in neuropsychiatric disorders and exploring therapeutic avenues for conditions such as schizophrenia. -
CHI3L1 Inhibitor
CHI3L1-IN-1 is a selective inhibitor of Chitinase-3-like protein 1 (CHI3L1), also known as YKL-40, with an IC50 of 50 nM. This compound exhibits additional effects by inhibiting the hERG channel with an IC50 of 2.3 μM. CHI3L1-IN-1 is valuable for research applications focused on the roles of CHI3L1 in inflammation and cancer, offering insights into its potential as a biomarker and therapeutic target. -
M-type K+ current Inhibitor
Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology. -
Kv1.3 Inhibitor
Margatoxin is a highly selective inhibitor of the voltage-gated potassium channel Kv1.3, with a binding affinity (Kd) of 11.7 pM. It also exhibits inhibitory effects on Kv1.2 (Kd = 6.4 pM) and Kv1.1 (Kd = 4.2 nM). This 39-amino-acid peptide, derived from the venom of Centruroides margaritatus, is extensively utilized in ion channel research to study the role of Kv1.3 in various physiological and pathophysiological processes. -
Kv1.3 Inhibitor
Dalazatide is a potent inhibitor of the Kv1.3 potassium channel, specifically designed for research applications in autoimmune diseases. This peptide has shown efficacy in the modulation of immune responses, making it a valuable tool for studying conditions such as multiple sclerosis, lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease. Its role in Kv1.3 inhibition provides insights into the pathophysiology of these diseases and potential therapeutic avenues. -
Sodium Current Inhibitor
Eleclazine hydrochloride is a selective inhibitor of the cardiac late sodium current, exhibiting an IC50 value of less than 1 μM, along with a weaker inhibitory effect on potassium current (IC50 approximately 14.2 μM). This compound demonstrates therapeutic potential by providing protection against autonomically induced atrial premature beats, repolarization alternans, heterogeneity, and atrial fibrillation in porcine models. Eleclazine hydrochloride is applicable in the study of cardiac arrhythmias and their underlying mechanisms. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride monohydrate is a potent sodium channel inhibitor that reversibly blocks sodium ion influx, thereby disrupting impulse conduction in nerve fibers. Additionally, it inhibits the K2P potassium channel TREK-1 with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is widely utilized for regional anesthesia and in the management of neuropathic pain in vivo, making it a valuable reagent in pain research and therapeutic applications. -
KCNQ2 Inhibitor
ML252 is a selective inhibitor of the KCNQ2 (Kv7.2) ion channel, exhibiting an IC50 of 69 nM for KCNQ2, along with lower inhibitory effects on KCNQ1, KCNQ2/Q3, and KCNQ4. This compound also demonstrates inhibition of key Cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP3A4, and CYP2D6, with IC50 values ranging from 3.9 nM to 19.9 nM. ML252 is notable for its ability to penetrate the blood-brain barrier, making it a valuable tool for investigating neuronal function and related disorders. -
Potassium Channel Inhibitor
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM. This compound exhibits significant immunosuppressive activity, effectively inhibiting the proliferation of human and rat myelin-specific effector memory T cells in vitro. Its specificity for Kv1.3 makes it a valuable tool for studying autoimmune disorders and T cell-mediated responses in research applications. -
KATP Channel Inhibitor
Cibenzoline is a KATP channel inhibitor targeting the pore-forming subunit Kir6.2, exhibiting an IC50 of 22.2 μM. This compound also inhibits cardiac ion currents IKr and IKs, with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is primarily utilized in the investigation of cardiac diseases, and it has been shown to induce hypoglycemia, making it relevant for studies related to glucose metabolism and endocrine functions. -
SLO3 Inhibitor
VU0546110 is a selective inhibitor of the sperm-specific potassium channel SLO3, exhibiting an IC50 of 1.287 μM for SLO3 in HEK293 cells and a more modest IC50 of 59.80 μM for SLO1. This compound effectively blocks both heterologous SLO3 currents and endogenous K+ currents in human sperm, leading to the cessation of sperm hyperpolarization, acrosome reaction induction, and hyper-activated motility. VU0546110 is of particular interest in reproductive biology research due to its potential contraceptive applications. -
Potassium Channel Inhibitor
N-Acetylprocainamide is a potassium channel inhibitor that functions as a class III antiarrhythmic agent. By blocking K+ channels, it effectively modulates cardiac action potentials, making it relevant in the study of arrhythmias. This compound serves as a valuable tool in cardiac electrophysiology research and associated therapeutic investigations. -
Kir6.1/SUR2B KATP channel inhibitor
VU0542270 is a selective inhibitor of the vascular Kir6.1/SUR2B KATP channel, demonstrating an IC50 value of 100 nM. It exhibits minimal activity against other members of the Kir channel family, with an IC50 greater than 30 μM for nine variants. This compound is valuable for investigating the role of KATP channels in cardiovascular disease and exploring potential therapeutic strategies. -
TREK-1 Inhibitor
PE 22-28 is a potent TREK-1 inhibitor with an IC50 value of 0.12 nM, demonstrating its efficacy in modulating TREK-1 activity. This 7-amino-acid peptide serves as a core sequence for generating analogs through chemical modifications or amino acid substitutions. PE 22-28 is relevant for research into depression, offering insights into the role of TREK-1 in mood regulation and potential therapeutic interventions. -
TASK-1 Inhibitor
AVE1231 is a selective inhibitor of the two-pore potassium channel TASK-1, effectively blocking carbamoylcholine chloride-activated IKACh with an IC50 of 8.4 μM. This compound plays a crucial role in the study of electrophysiological processes, making it valuable for research focused on cardiac arrhythmias and atrial fibrillation. Its ability to modulate potassium ion currents offers insights into the mechanisms underlying these cardiovascular conditions. -
Kir4.1/5.1 Inhibitor
VU6036720 is a selective inhibitor of Kir4.1/5.1 channels, exhibiting potent in vitro activity with an IC50 of 0.24 μM. This compound is valuable for investigating the physiological roles of Kir4.1/5.1 in both brain and kidney tissues. Its specificity makes it an essential tool for studies focused on ion channel modulation in neurological and renal research. -
TRESK/TASK-1 Inhibitor
A2793 is a selective inhibitor of the TWIK-related acid-sensitive K+ channels, TASK-1 and TRESK. With an IC50 of 6.8 μM for mTRESK, this reagent demonstrates significant activity against TRESK while exhibiting only moderate effects on TREK-1 and TALK-1. A2793 is valuable for research applications focusing on ion channel regulation and neurological studies. -
TRESK Inhibitor
A2764 dihydrochloride is a potent and selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), exhibiting moderate inhibitory effects on TREK-1 and TALK-1 channels. This compound demonstrates increased sensitivity to activated mTRESK channels, with an IC50 value of 6.8 μM. A2764 dihydrochloride effectively induces cell depolarization and enhances excitability in native cells, making it a valuable tool for investigating the role of TRESK channels in migraine pathophysiology and nociceptive signaling. -
TRAAK Inhibitor
RU-TRAAK-2 is a selective inhibitor of the TRAAK (TWIK-related arachidonic acid-stimulated K+ channel) that demonstrates complete reversibility in its inhibitory action. It shows no activity against other potassium channels, including Kv1.2, Slo1, and GIRK2, ensuring specificity in experimental applications. Additionally, RU-TRAAK-2 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool in chemical biology for labeling and tagging biomolecules. This compound is primarily utilized in research focusing on ion channel regulation and signaling pathways. -
TREK-1 Inhibitor
TKIM is a selective inhibitor of the TREK-1 channel, exhibiting an IC50 of 2.96 μM. By binding to the pocket of the intermediate (IM) state of TREK-1, TKIM modulates ion channel activity. This compound is valuable for investigations into the physiological roles of TREK-1 in neurobiology and cardiovascular research, as well as potential therapeutic applications in pain and mood disorders. -
KV1.3 Inhibitor
KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, exhibiting IC50 values of 230 nM in Ltk cells and 26.12 nM in PHA-activated T-lymphocytes. This compound disrupts intracellular Ca2+ signaling, leading to notable inhibition of T-cell activation, proliferation, and colony formation. KV1.3-IN-1 is an essential tool for research on T-cell biology and the modulation of immune responses. -
TREK Inhibitor
ONO-TR-772 is a selective TREK inhibitor with an IC50 value of 15 nM. This compound has been shown to enhance recognition memory in the MK-801-stimulated novel object recognition (NOR) mouse model. ONO-TR-772 is valuable in research pertaining to cognitive impairment and related neurological diseases. -
KV7 Activator/NaV Inhibitor
E0199 is a potent dual-target KV7 activator and NaV inhibitor, specifically enhancing KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels while inhibiting NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. This compound demonstrates significant analgesic properties in a chronic constriction injury mouse model, effectively managing neuropathic pain without adversely impacting cardiac and skeletal muscle ion channels. E0199 serves as a valuable tool for research in neuropathic pain mechanisms and therapeutic strategies. -
Potassium Channel Inhibitor
VU625 is a selective inhibitor of the inward rectifier potassium channel 1 (AeKir) in the Aedes aegypti mosquito, exhibiting an IC50 of 96.8 nM in HEK293 cells. This compound demonstrates potential for development as a novel insecticide, targeting critical pathways in mosquito physiology. Its specificity for AeKir makes it a valuable tool for research aimed at controlling mosquito populations and studying potassium channel function. -
KV1.3 Inhibitor
cis-KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, specifically designed to target this ion channel in cellular systems. At a concentration of 10 μM, cis-KV1.3-IN-1 demonstrates a 25.53% inhibition of KV1.3 activity in Xenopus oocytes expressing human hKV1.3. This compound is valuable for research into immunological responses and therapies, particularly in relation to autoimmune diseases where KV1.3 channels play a critical role. -
Potassium Channel Inhibitor
Charybdotoxin is a 37-amino acid peptide that selectively inhibits potassium channels. Its primary mechanism involves blocking voltage-gated K+ channels, leading to altered neuronal excitability and muscle contraction. This compound is useful in research applications focused on neurophysiology, cardiac function, and ion channel studies, providing insights into the role of potassium channels in physiological and pathological processes. -
ROMK Inhibitor
MK-8153 is a highly selective and orally active inhibitor of the renal outer medullary potassium channel (ROMK), demonstrating an IC50 of 5 nM for ROMK electrophysiology. This compound's potent inhibitory action makes it suitable for research applications related to diuresis and atriuresis. Its specificity towards ROMK provides a valuable tool for studying renal function and potassium homeostasis in various biological contexts. -
Potassium Channel Inhibitor
Guanfu base G is a potassium channel inhibitor derived from Aconitum coreanum. It effectively inhibits the HERG channel current, exhibiting an IC50 value of 17.9 μM. This compound is primarily utilized in research applications focused on cardiac arrhythmias and the modulation of ion channel activity.
