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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
AMPA Receptor Inhibitor
Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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Proton pump inhibitor
Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. -
Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. -
proton pump inhibitor
Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid. -
PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. -
ATPase Inhibitors
Omeprazole is a cell-permeable, selective proton pump inhibitor. -
CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy. -
Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
protein tyrosine phosphatases inhibitor
Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue. -
Calcium Channel inhibitor
Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis. -
SGLT2 inhibitor
PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2. -
noradrenalin transporters inhibitor
Desipramine hydrochloride is a tricyclic antidepressant that is a selective inhibitor of noradrenalin transporters (Ki values are 4, 61 and 78720 nM for NET, SERT and DAT transporters respectively).
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Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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TRPV1 antagonist and TNF-alpha production inhibitor
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor. -
CRM1-selective inhibitor
Selinexor trans-isomer is a trans-isomer of Selinexor or KPT-330, which is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells. -
VMAT-2 inhibitor
Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). -
Potassium Channel inhibitor
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. -
VDAC Inhibitor
DIDS sodium salt is a potent inhibitor of voltage-dependent anion channels (VDAC1) and also targets the ABCA1 transporter. This compound effectively disrupts RAD51-mediated homologous pairing and strand exchange reactions, making it valuable for studying DNA repair mechanisms. Additionally, DIDS is known to inhibit anion exchange and interfere with caspase-3 and -9 activation, facilitating its application in cancer research and apoptosis studies. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
Autophagy Inhibitor
Reserpine acts as an inhibitor of vesicular monoamine transporter 2 (VMAT2), thereby influencing neurotransmitter storage and release. This compound is widely utilized in research studies focusing on autophagy inhibition and its implications in various neurodegenerative disorders. Additionally, reserpine's effects on monoamine levels make it a valuable tool in the investigation of psychiatric conditions and the biochemical pathways involved in these diseases. -
Bacterial Inhibitor
Probenecid is a selective inhibitor of bacterial growth, primarily targeting pannexin 1 channels, while also exhibiting activity as a TRPV2 channel agonist. Its ability to modulate ion channel activity makes it valuable for research into pain pathways and inflammatory responses. Probenecid is commonly used in studies investigating the role of TRPV2 in nociception and as a tool in exploring bacterial resistance mechanisms. -
IL-1 Inhibitor
Diacerein is a potent IL-1 inhibitor that functions by reducing the production of IL-1 converting enzyme, thereby inhibiting the activation of IL-1β and its downstream signaling pathways. This compound exhibits significant anti-inflammatory and anti-rheumatic properties, making it useful for various research applications, including studies on osteoarthritis and the management of bronchospasm and airway inflammation in asthmatic models. Diacerein is recognized as a slow-acting drug for symptomatic relief of osteoarthritis, facilitating insights into long-term therapeutic strategies. -
L-glutamate Uptake Inhibitor
Evans Blue is a potent inhibitor of L-glutamate uptake through the membrane-bound excitatory amino acid transporter (EAAT). This compound effectively inhibits L-glutamate and kainate receptor-mediated currents, making it valuable for research into neurophysiological processes. Additionally, due to its strong affinity for serum albumin, Evans Blue serves as a high molecular weight protein tracer and is widely used to investigate blood-brain barrier (BBB) permeability. -
VMAT2 Inhibitor
Reserpine hydrochloride is a potent inhibitor of the vesicular monoamine transporter 2 (VMAT2). It is primarily utilized in research to study neurotransmitter release and its implications in neurodegenerative diseases and mental health disorders. By inhibiting VMAT2, Reserpine hydrochloride disrupts the storage of monoamines, allowing for investigation into their effects on various physiological and pathological processes. -
SERCA2 Inhibitor
COX-2-IN-55 is a selective SERCA2 inhibitor that exhibits promising anticancer properties, with a unique profile derived from a Celecoxib analog. This compound enhances caspase-3 cleavage and elevates DR5 levels, leading to the activation of GRP78, which contributes to the repression of triple-negative breast cancer (TNBC) progression. Additionally, COX-2-IN-55 reduces angiogenic markers such as VEGF-α and IL-8, effectively inhibiting microvessel formation and supporting its potential utility in cancer research applications. -
P-glycoprotein Inhibitor
1-Monopalmitin, also known as Glyceryl palmitate, functions as an inhibitor of P-glycoprotein (P-gp) and modulates the PI3K/Akt signaling pathway. It has been shown to induce G2/M phase arrest and promote caspase-dependent apoptosis in cancer cells, while also downregulating inhibitor of apoptosis proteins (IAPs). Additionally, 1-Monopalmitin enhances drug accumulation in intestinal Caco-2 cells by inhibiting P-gp activity and has demonstrated the ability to induce protective autophagy and apoptosis in lung cancer cells with an IC50 of 50-58 μg/mL, exhibiting low toxicity towards normal cells. -
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. -
SMARCA4/SMARCA2 ATPase inhibitor
FHD-286 is a selective, orally active inhibitor of the SMARCA4/SMARCA2 (BRG1/BRM) ATPase. It holds potential for research into BAF (BRG1/BRM-associated factor)-related disorders, including acute myeloid leukemia. -
SMARCA4/SMARCA2 ATPase Inhibitor
FHT-1015 is a selective allosteric inhibitor of SMARCA4 (BRG1) and SMARCA2 (BRM), with IC₅₀ values of 4 nM and 5 nM, respectively. It binds to an allosteric site, inducing conformational changes that inhibit the ATPase activity of BRG1/BRM. FHT-1015 disrupts tumor cell growth and migration and is applicable in research on uveal melanoma and hematologic malignancies.
