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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
PDE4 Inhibitor
L-869298 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 value of 0.5 nM for the PDE4A isoform. This compound exhibits minimal activity against the hERG potassium channel, making it a valuable tool for studies focused on inflammation, neurodegeneration, and other PDE4-related pathways. Its specificity and efficacy make it a suitable candidate for research applications in therapeutic development targeting PDE4-mediated signaling. -
BRG1/BRM ATPase Inhibitor
BRM/BRG1 ATP Inhibitor-2 is a selective inhibitor of BRG1 and BRM ATPase activity, targeting the SWI/SNF chromatin remodeling complexes. This compound is valuable for investigating the molecular implications of BAF-related disorders, including cancer and developmental syndromes. Its mechanism of action enables researchers to explore the role of ATP-dependent chromatin remodeling in gene expression regulation and cellular differentiation. -
SMARCA2 ATPase Inhibitor
SMARCA2-IN-10 is a selective inhibitor of the SMARCA2 ATPase domain, with an IC50 value of 17.676 μM. This compound has been shown to induce cell death in tumors lacking SMARCA4, making it a valuable tool for investigating SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma. Its targeting of the SMARCA2 ATPase offers significant potential for advancing research in these cancer types. -
DPP8/9 Inhibitor
DPP8/9-IN-2 is a selective inhibitor of dipeptidyl peptidase 8 and 9 (DPP8/DPP9) with potent inhibitory activity, exhibiting IC50 values of 0.22 nM and 3 nM, respectively. This compound has been implicated in research related to tumor biology and other pathological conditions. Notably, DPP8/9-IN-2 demonstrates certain cardiotoxicity, indicated by its IC50 values of 0.7 μM for the hERG potassium channel, 29.0 μM for the Nav1.5 sodium channel, and 27.7 μM for the Cav1.2 calcium channel. -
TRPA1 Inhibitor
Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms. -
Parasite Inhibitor
Milbemycin oxime is an orally active macrolide that serves as a potent inhibitor of parasite activity. This compound, a mixture of oxime derivatives related to milbemycin A4 and A3, selectively binds to glutamate-gated chloride channels, leading to paralysis and death of various intestinal nematodes and lung/heart worms. It is widely utilized in research focused on antiparasitic drug development and mechanisms of parasitic resistance. -
P-gp Inhibitor
Milbemycin A4 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing multidrug resistance in tumor cells. As a member of the macrolide antibiotic family, Milbemycin A4 displays significant insecticidal and acaricidal properties. This compound is valuable for research focused on overcoming chemotherapy resistance and studying P-gp-related mechanisms in cellular drug transport. -
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. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
p97 ATPase Inhibitor
p97-IN-2 is a selective inhibitor of the p97 ATPase, with an IC50 of 0.6 μM. This compound effectively inhibits the proliferation of cancer cell lines, including HCT15 (IC50 = 1.1 μM) and SW403 (IC50 = 0.8 μM). p97-IN-2 serves as a valuable tool for investigating the role of p97 in cancer biology and therapeutic applications. -
ERAD Inhibitor
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor that functions as a direct binder to VDAC1, VDAC2, and VDAC3. It demonstrates an IC50 of 1.02 μM for inhibiting ERAD and a Kd of 3.13 μM for binding human VDAC1. By disrupting cellular calcium homeostasis and enhancing VDAC1-IP3R coupling, NCATS-SM0225 activates the PERK pathway and selectively induces apoptosis in cancer cells. This reagent is valuable for investigating cancer biology, particularly in melanoma, as well as exploring the underlying mechanisms of ERAD and calcium homeostasis regulation. -
Serotonin And Norepinephrine Reuptake Inhibitor
Milnacipran is an orally active serotonin and norepinephrine reuptake inhibitor that primarily targets the monoamine transporters responsible for neurotransmitter reuptake. It demonstrates high affinity for the norepinephrine transporter and serotonin transporter, with Ki values of 31 nM and 8.5 nM, respectively. Milnacipran exhibits antidepressant, anxiolytic, and analgesic properties, and has been shown to inhibit pERK1/2 activation. This compound is applicable in the study of major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. -
RAD51 Inhibitor
DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications. -
Proton Pump Inhibitor
Ilaprazole sodium hydrate is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, exhibiting an IC50 value of 6 μM in rabbit parietal cell preparations. This compound is primarily utilized in research related to gastric ulcers, providing insights into gastric acid secretion and its regulation. In addition, Ilaprazole sodium hydrate demonstrates inhibitory activity against TOPK (T-lymphokine-activated killer cell-originated protein kinase), making it a valuable tool for studies on cellular signaling pathways and cancer research. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
FTO Inhibitor
Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes. -
Aliostericeffect for Myosin ATPase 13 Inhibitor
Diazobenzenesulfonic acid, also known as 4-Sulfobenzenediazonium, functions as an allosteric inhibitor of myosin ATPase 13. This compound has significant biological activity by modulating the enzyme's function, thereby influencing muscle contraction mechanisms. It is primarily utilized in research applications aimed at understanding myosin-related pathways and exploring potential therapeutic targets for muscle-related diseases. -
Cardiac Myofibrillar ATPase Inhibitor
DN-F01 is a potent inhibitor of cardiac myofibrillar ATPase, exhibiting a strong calcium-dependent activity with an IC50 value of 11 ± 4 nmol/L. This compound serves as a valuable tool in studying cardiac muscle contractility and ATPase regulation. Its ability to selectively inhibit cardiac myofibrillar ATPase makes it suitable for research in cardiovascular physiology and related pathologies. -
Myosin ATPase Inhibitor
Myosin-IN-2 is a potent Myosin ATPase inhibitor, demonstrating an IC50 of 1.06 μM. This compound plays a critical role in research focused on heart diseases, particularly hypertrophic cardiomyopathy (HCM). By selectively inhibiting Myosin ATPase activity, Myosin-IN-2 provides valuable insights into the mechanisms underlying cardiac function and related pathological conditions. -
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. -
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. -
H+, K+-ATPase Inhibitor
Esomeprazole magnesium salt is a selective inhibitor of the H+, K+-ATPase enzyme in gastric parietal cells, functioning as an effective proton pump inhibitor. This compound demonstrates significant biological activity by reducing gastric acid secretion. It is primarily utilized in research related to gastroesophageal reflux disease, exploring its therapeutic potential and mechanisms of action in acid-related disorders. -
Proton Pump Inhibitor
S-Pantoprazole sodium trihydrate is a potent proton pump inhibitor that effectively reduces gastric acid secretion. It is primarily utilized in the treatment of conditions associated with excessive gastric acid production, such as gastroesophageal reflux disease (GERD) and peptic ulcers. Its mechanism of action involves the irreversible inhibition of the H+/K+ ATPase enzyme in gastric parietal cells, providing therapeutic benefits in managing acid-related disorders. -
Na+-V-ATPase Inhibitor
V-161 is an orally active inhibitor of Na+-V-ATPase, exhibiting an IC50 of 144 nM. This compound effectively inhibits the growth of Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline conditions, with a minimum inhibitory concentration (MIC) of 4 µg/mL for both bacterial strains. In vivo studies demonstrate that V-161 significantly reduces VRE colonization in the mouse small intestine, making it a valuable tool for research into antimicrobial resistance and gut microbiota interactions. -
Proton Pump Inhibitor
Lansoprazole sulfide-d4 is a deuterium-labeled form of Lansoprazole sulfide, a bioactive metabolite of the proton pump inhibitor Lansoprazole. This compound exhibits significant activity against Mycobacterium tuberculosis, demonstrating IC50 values of 0.59 μM intracellularly and 0.46 μM in broth. It is a valuable tool for research into anti-tubercular therapies and the pharmacokinetics of proton pump inhibitors. -
CGRP/TRPV1 Inhibitor
Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders. -
OCT1 Inhibitor
Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) selectively inhibits the organic cation transporter OCT1, with an IC50 value of 6.6 μM. This compound also acts as a competitive inhibitor of tyrosine hydroxylase, reducing dopamine biosynthesis with an IC50 of 20.7 μM in PC12 cells. Hydrastine is particularly relevant for research into Parkinson's disease, as it may induce neuronal toxicity through mitochondrial dysfunction and has the potential to exacerbate apoptosis when used in conjunction with L-DOPA. -
μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor
ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation. -
Sodium Channel Inhibitor
Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology. -
EBP Inhibitor
EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders. -
Calcium Channel Inhibitor
Ethacrynic acid sodium is an effective calcium channel inhibitor that primarily targets L-type voltage-dependent and store-operated calcium channels. This compound exhibits diuretic properties and significantly modulates glutathione S-transferases (GSTs) while inhibiting the NF-kB signaling pathway. Ethacrynic acid sodium demonstrates anti-inflammatory activity, evidenced by its ability to reduce retinoid-induced ear edema in murine models, making it a valuable tool in research focused on inflammation and airway smooth muscle relaxation. -
Calcium Channel Inhibitor
Levamlodipine hydrobromide is a calcium channel inhibitor with notable antioxidant and vasodilatory properties. This compound has been shown to reduce serum malondialdehyde (MDA) levels while increasing superoxide dismutase (SOD) activity, thus improving oxidative stress responses. It is appropriate for research applications related to vascular dementia, hypertension, and cerebrovascular diseases. -
TLR4/HCN Inhibitor
HCN-IN-1 is a TLR4 inhibitor and modulator of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, specifically targeting HCN2 and HCN4. It effectively inhibits TLR4-mediated signaling, evidenced by reduced alkaline phosphatase activity. HCN-IN-1 modulates HCN2 currents by shifting the voltage-dependent activation to hyperpolarized potentials and slowing activation kinetics, while also blocking currents through HCN4 channels. This compound demonstrates significant analgesic, anti-inflammatory, and anti-anginal properties, making it valuable for research into inflammatory pain, neuropathic pain, heart failure, and related inflammatory conditions. -
TRPV1 Inhibitor
(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels. -
TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
