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Catalog No.
Product Name
Application
Product Information
Citations
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P-gp inhibitor
Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
CaCCs Inhibitor
CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells). -
TMEM16A Inhibitor
T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. -
ATPase and GTPase inhibitor
Etidronate Disodium is a bisphosphonate bone resorption inhibitor. -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. -
P-Glycoprotein Inhibitor
(R)-Verapamil hydrochloride is an orally active P-Glycoprotein inhibitor that effectively blocks MRP1-mediated transport. This compound induces apoptosis and inhibits L-type calcium channels, including BZPcc, DHPcc, and PLLcc. Additionally, (R)-Verapamil hydrochloride demonstrates potential anti-septic shock and anti-diabetic effects, making it suitable for a range of research applications in cellular signaling and drug transport studies. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
PP Inhibitor
Pantoprazole sodium hydrate is a potent proton pump inhibitor (PPI) that targets the H+/K+-ATPase enzyme. With an IC50 value of 6.8 μM, it exhibits significant anti-secretory and anti-ulcer properties. This compound has been demonstrated to enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable reagent for studies involving cancer treatment and gastrointestinal disorders. -
F0F1-ATPase Inhibitor
Apoptolidin is a polyketide compound that selectively inhibits the mitochondrial F0F1-ATPase. It has been demonstrated to induce apoptotic cell death specifically in cells transformed with adenovirus type 12 oncogenes, such as ElA, with an IC50 of 10-17 ng/ml. Apoptolidin serves as a valuable tool for studying apoptotic mechanisms and mitochondrial function in cancer research. -
Kv2.1 Inhibitor
Kv2.1-IN-1 is a selective inhibitor of the Kv2.1 potassium channel, demonstrating a potent inhibitory activity with an IC50 of 0.07 μM. It exhibits over 130-fold selectivity against other potassium, sodium, and calcium channels. Kv2.1-IN-1 has been shown to reduce H2O2-induced apoptosis in HEK293 cells and provides significant neuroprotective effects in models of middle cerebral artery occlusion (MCAO) in rats. This compound is useful for research into ischemic stroke and related neurological conditions. -
V-ATPase Inhibitor
RSC-1255 is a potent and selective inhibitor of Vacuolar H⁺-ATPase (V-ATPase), demonstrating a binding affinity with a Kd of 23 nM. This compound exhibits preferential cytotoxicity towards KRAS-mutant cancer cells, particularly those harboring KRASG13D and KRASG12V mutations. RSC-1255 effectively induces apoptosis while inhibiting lysosomal acidification, autophagy, and macropinocytosis. It serves as a valuable tool for researching KRAS-driven lung and colon cancers. -
ATPase Inhibitor
ATPase-IN-3 is an ATPase inhibitor that demonstrates gastroprotective effects in models of ethanol-induced gastric ulcers. Its mechanism of action involves the modulation of anti-apoptotic pathways through the upregulation of BCL-2 and the activation of tumor suppressor protein P53. This compound is valuable for research applications aimed at investigating gastric ulcer pathophysiology and potential therapeutic interventions. -
P-gp Inhibitor
RMS3 is a tetrandrine analogue that functions as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits significant antiproliferative and cytotoxic effects on various cancer cell lines. Notably, RMS3 induces PARP cleavage, which is indicative of cells undergoing apoptosis. Its strong anticancer properties make RMS3 a valuable tool for cancer research and therapeutic studies. -
P-gp Inhibitor
RMS5 is a potent P-glycoprotein (P-gp) inhibitor, derived from a tetrandrine analogue. It exhibits significant antiproliferative and cytotoxic effects on cancer cells, contributing to its strong anticancer properties. Additionally, RMS5 has been observed to reduce the expression of anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1 while inducing PARP cleavage, a hallmark of apoptosis. This compound is valuable for research applications focusing on cancer therapeutics and the modulation of multidrug resistance. -
P-gp Inhibitor
(R)-OY-101 is an orally active and selective inhibitor of P-glycoprotein (P-gp). This compound enhances the sensitivity of tumors to anticancer agents by reversing drug resistance and promoting apoptosis. It has valuable applications in cancer research, particularly in studies focused on overcoming multidrug resistance and improving therapeutic efficacy. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
KATP Inhibitor
Tolbutamide is an orally active KATP inhibitor that primarily targets ATP-sensitive potassium channels. It is known to inhibit cell proliferation and stimulate the exocytosis of glucagon, while also reducing fetal lethality in murine models. This compound is utilized in diabetes research to explore mechanisms of insulin secretion and glucose metabolism. -
Proton Pump Inhibitor
Omeprazole sodium is a proton pump inhibitor (PPI) that effectively reduces gastric acid secretion, making it useful in treating acid-related gastrointestinal disorders. In addition to its primary role, omeprazole sodium competitively inhibits CYP2C19 with a Ki value ranging from 2 to 6 μM, which may influence drug metabolism. This compound also displays antibacterial activity against both Gram-positive and Gram-negative bacteria, and it serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production. Its diverse biological activities make it a valuable tool for research in pharmacology and microbiology. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
ABCG2/BCRP Inhibitor
Triclabendazole sulfoxide is an ABCG2/BCRP inhibitor that serves as the primary plasma metabolite of Triclabendazole. This compound demonstrates significant anti-parasitic activity and is useful in research applications focusing on the modulation of drug transport mechanisms in cellular assays. It contributes to studies investigating the role of ABCG2/BCRP in drug resistance and pharmacokinetics. -
HSP70 ATPase Inhibitor
Displurigen (NSC375009) is an HSP70 ATPase inhibitor that specifically targets HSPA8, disrupting the pluripotency of human embryonic stem cells. This compound effectively inhibits the ATPase activity of HSP70 with an IC50 of 225 μM, making it a valuable tool for research in stem cell biology and differentiation processes. Its mechanism of action provides insights into cellular signaling pathways related to stem cell maintenance and development. -
ASH ATPase Activity Inhibitor
SEW84 is a potent inhibitor of Aha1-stimulated Hsp90 (ASH) ATPase activity, demonstrating an IC50 of 0.3 μM. This compound is valuable for investigating the role of Hsp90 in protein deposition disorders and offers insights into the underlying mechanisms of these diseases. Additionally, SEW84 may serve as a tool for studying Hsp90's involvement in cellular stress responses and protein folding pathways. -
P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
Cytochrome P450 Inhibitor
Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections. -
Parasite Inhibitor
Ep vinyl quinidine, an epi-vinyl stereoisomer of Quinidine, serves as a targeted inhibitor of parasitic activity. This compound exhibits significant potential in malaria research, leveraging its capabilities as a selective cytochrome P450db inhibitor. Additionally, it functions as a potassium channel blocker with an IC50 of 19.9 μM, positioning it as a valuable tool for investigating anti-parasitic mechanisms and therapeutic interventions. -
HCV Inhibitor
Vedroprevir is a potent inhibitor of the HCV NS3/4A protease, demonstrating an IC50 of 3.2 nM. In addition to its antiviral activity, Vedroprevir also inhibits the breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM, as well as P-glycoprotein (P-gp), MRP1, and MRP2 with IC50 values of 34 μM, 14.9 μM, and 12 μM, respectively. These characteristics make Vedroprevir valuable for research in hepatitis C and multidrug resistance cancer studies. Its favorable pharmacokinetic profile has been observed in preclinical models, including rats and dogs. -
V-ATPase/HIV-1 Inhibitor
Diphyllin is a potent inhibitor of vacuolar H+-ATPase (V-ATPase) with an IC50 of 17 nM, and also acts as an HIV-1 inhibitor with an IC50 of 0.38 μM. This compound effectively disrupts the acidification of osteoclast lysosomes, leading to significant inhibition of osteoclast-mediated bone resorption while leaving osteoblastic bone formation unaffected. Diphyllin is valuable for investigating bone metabolism-related diseases and exploring therapeutic avenues for conditions characterized by excessive bone resorption. -
H+, K+-ATPase Inhibitor
Esomeprazole hemistrontium is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by targeting the H+, K+-ATPase enzyme in parietal cells. This compound is particularly valuable for research applications related to symptomatic gastroesophageal reflux disease. -
Na+/K+ ATPase Inhibitor
Chamigrenol is an inhibitor of the Na+/K+ ATPase, exhibiting an IC50 value of 15.9 μg/mL. This compound demonstrates significant antibacterial activity against both Gram-positive and Gram-negative bacteria, with the exception of Escherichia coli, showing minimum inhibitory concentration (MIC) values of 50 µg/mL. Chamigrenol is valuable for research in microbiology and the development of novel antimicrobial agents. -
Na+/K+-ATPase Inhibitor
(-)-γ-Cuparenol is a sesquiterpene compound that acts as an inhibitor of Na+/K+-ATPase, with an IC50 value of 23.6 μg/mL in porcine models. It has demonstrated the ability to reduce phytohemagglutinin (PHA)-induced activation of NF-AT and NF-κB in Jurkat cells, indicating potential applications in immunoregulation. Additionally, (-)-γ-Cuparenol exhibits antibacterial activity against certain Gram-positive and some Gram-negative bacteria, as well as weak inhibitory effects on Candida albicans. This compound is relevant for research exploring cardiovascular diseases and bacterial infections. -
H+, K+-ATPase Inhibitor
Esomeprazole (S-Omeprazole) is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by specifically inhibiting the H+, K+-ATPase enzyme in parietal cells of the stomach lining. This compound is valuable in research related to gastroesophageal reflux disease and studies investigating acid secretion mechanisms. -
Proton Pump Inhibitor
(S)-Lansoprazole is a proton pump inhibitor that effectively reduces gastric acid secretion by inhibiting the proton pump in the stomach lining. This compound demonstrates significant potential for therapeutic applications in acid-related gastrointestinal disorders such as gastroesophageal reflux disease (GERD) and peptic ulcers. Additionally, as a neutral sphingomyelinase (N-SMase) inhibitor, it has been investigated for its role in modulating exosome release and may offer insights into neuroprotective research. -
H+, K+-ATPase Inhibitor
Esomeprazole potassium salt is a potent H+, K+-ATPase inhibitor, primarily functioning as a proton pump inhibitor. It effectively reduces gastric acid secretion by targeting the H+, K+-ATPase enzyme in gastric parietal cells. This compound is valuable for research applications focusing on symptomatic gastroesophageal reflux disease and related gastrointestinal disorders. -
ATPase/Bacterial Inhibitor
Dihydronovobiocin is a bacterial inhibitor that targets ATPase activity by binding to the GyrB subunit of DNA gyrase. This compound is useful for investigating the interactions between coumarin antibiotics, such as Novobiocin, Chlorobiocin, and Coumermycin, and their effects on DNA gyrase function. Dihydronovobiocin also has potential applications in the study of bacterial infections, facilitating research into the mechanisms of antibiotic action and resistance. -
Potassium Channel Inhibitor
Naluzotan hydrochloride is a selective potassium channel inhibitor that primarily functions as an amidosulfonamide 5-HT1A agonist, exhibiting an IC50 of approximately 20 nM and a Ki value of 5.1 nM. This compound demonstrates notable activity in modulating neurotransmitter pathways, making it a valuable tool for research into anxiety and depression treatments. Additionally, naluzotan hydrochloride acts as a weak hERG K+ channel blocker with an IC50 of 3800 nM, highlighting its potential relevance in cardiac safety assessments. -
Noradrenalin Reuptake Inhibitor
Beloxepin is a synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. It demonstrates selective inhibition with approximately 100-fold lower affinity for other monoamine transporters. Beloxepin exhibits significant antidepressant and analgesic properties, making it useful for research centered on mood disorders and pain management. -
ATPase Inhibitor
ATPase-IN-6 is a H+/K+-ATPase inhibitor and a prazole derivative. It exhibits significant antiviral activity against a range of viruses, including HIV-1 and SARS-CoV-2. This compound is useful for research investigating antiviral mechanisms and potential therapeutic strategies for viral infections. -
TrpAB Inhibitor
BRD-4592 is an allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase (TrpAB), specifically targeting the α-β-subunit interface. It demonstrates potent inhibitory activity, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit. This compound is valuable for research applications aimed at elucidating the role of tryptophan metabolism in tuberculosis and exploring novel therapeutic strategies against Mycobacterium tuberculosis. -
Proton Pump Inhibitor
AHR-9294 is a potent inhibitor of the H+ pump enzyme, specifically targeting H, K-ATPase. This compound effectively inhibits gastric acid secretion in vivo, making it valuable for research related to gastrointestinal physiology and the treatment of acid-related disorders. Its mechanism of action supports studies exploring proton pump inhibition and related therapeutic applications. -
ATPase Inhibitor
Apicularen A is a macrolide that selectively inhibits vesicular ATPases, targeting ATPase activity in cellular processes. This compound has been isolated from the mucoid bacterium Chondrosporium spp. Its potent inhibitory effects make it a valuable tool for research applications focused on cellular transport mechanisms and metabolic regulation. -
CV-B3 2C ATPase Inhibitor
ATPase-IN-8 is a selective inhibitor of CV-B3 2C ATPase, exhibiting an IC50 of 1.4 μM. This compound demonstrates significant anti-enteroviral activity, particularly against coxsackievirus B3 (CV-B3) and enterovirus D68 (EV-D68). ATPase-IN-8 is suitable for research applications focusing on enteroviral infections and their molecular mechanisms. -
ASK1 Inhibitor
ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications. -
hERG Inhibitor
GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways.
