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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
AMPAR Inhibitor.
D15 is an AMPA receptor (AMPAR) endocytosis inhibitor derived from a 15 amino acid segment of dynamin. It inhibits the interaction of dynamin with amphiphysin 1 and 2, leading to a significant increase in AMPAR excitatory postsynaptic potential (EPSC) amplitude in medium spiny neurons (MSNs) within Sapap3 knockout mice. This peptide has valuable applications in the investigation of neuropsychiatric disorders and related signaling pathways. -
AMPA Receptor Inhibitor
AMPA-IN-1 is a potent inhibitor of the AMPA receptor, which is critical for fast excitatory synaptic transmission and synaptic plasticity in the brain. By modulating AMPA receptor activity, AMPA-IN-1 demonstrates potential for research into various central nervous system disorders, including epilepsy. This compound may provide valuable insights into therapeutic strategies targeting excitatory neurotransmission. -
AMPA Inhibitor
AMPA-IN-2 is a potent orally active inhibitor of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, efficiently crossing the blood-brain barrier. This compound demonstrates significant anti-epileptic effects by reducing neuronal excitability and attenuating glutamatergic transmission. AMPA-IN-2 is effective in the pentylenetetrazol model of epilepsy, making it a promising candidate for research in the field of epilepsy and related neuronal excitability disorders. -
Transporter Inhibitor
Pseudoisocyanine iodide, also known as 1,1'-Diethyl-2,2'-cyanine iodide, functions as an inhibitor of organic cation transporters (OCT1, OCT2, OCT3) and the plasma membrane monoamine transporter (PMAT). This compound exhibits antidepressant activity, making it valuable for research in mental health and neuropharmacology. Its ability to modulate transporter function positions it as a useful tool for studying mechanisms of neurotransmitter regulation and potential therapeutic interventions in mood disorders. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways. -
Monoamine Transporter Inhibitor
(+)-Tetrabenazine is a reversible inhibitor of the vesicular monoamine transporter 2 (VMAT-2). It exhibits a potency that is 10-fold greater for VMAT-2 than for VMAT-1, effectively restricting monoamine transport. This compound is primarily utilized in research focused on neurochemical pathways and the treatment of movement disorders, such as Huntington's disease and tardive dyskinesia, by regulating dopamine levels in the synaptic cleft. -
VMAT2 Inhibitor
Dihydrotetrabenazine (DHTBZ) is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2). By decreasing the monoamine content in presynaptic neurons, it plays a crucial role in the study of movement disorders. DHTBZ is essential for investigating the mechanisms underlying neurotransmitter regulation and offers potential insights into therapeutic strategies for neurological diseases. -
VMAT2 Inhibitor
(-)-Tetrabenazine is a specific inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound exhibits notable biological activity in the modulation of monoamine neurotransmitter levels, making it valuable for research in neuropharmacology and the study of movement disorders. Its role as a VMAT2 inhibitor can aid in the investigation of drug development for conditions such as Huntington's disease and other neurodegenerative disorders. -
VMAT2 Inhibitor
Tetrabenazine mesylate is a potent reversible inhibitor of the vesicular monoamine transporter VMAT2, with a Kd value of 1.34 nM. This compound is primarily used in research focused on hyperactive movement disorders, including Huntington's disease, due to its ability to modulate monoamine neurotransmitter release. Tetrabenazine mesylate serves as a valuable tool for studying the underlying mechanisms of these neurological conditions and evaluating potential therapeutic approaches. -
VMAT2 Inhibitor
Tetrabenazine Metabolite is a potent vesicular monoamine transporter 2 (VMAT2) inhibitor, exhibiting high affinity with a Ki of 13.4 nM. This active metabolite plays a crucial role in the modulation of monoamine neurotransmitter levels and is primarily investigated for its therapeutic potential in chorea associated with Huntington’s disease and other hyperkinetic disorders. Its mechanism of action supports ongoing research in neurological disease management and treatment strategies. -
VMAT2 Inhibitor
VMAT2-IN-2 tosylate is a potent inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound is essential for investigating the pathophysiology of conditions such as tardive dyskinesia, where dysregulation of neurotransmitter storage and release plays a critical role. VMAT2-IN-2 tosylate may provide valuable insights into therapeutic strategies and the development of treatment options for related neurological disorders. -
Monoamine Transporter Inhibitor
13-Hydroxyisobakuchiol is a selective inhibitor of monoamine transporters, primarily targeting the dopamine transporter (DAT) and norepinephrine transporter (NET) with IC50 values of 0.58 μM and 0.69 μM, respectively. In contrast, it exhibits significantly lower affinity for the serotonin transporter (SERT), with an IC50 of 312.02 μM. This compound is valuable for research applications related to neurodegenerative diseases, including Parkinson's disease, and mood disorders such as depression. -
Monoamine Transporter Inhibitor
Cendifensine is a monoamine transporter inhibitor that targets the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). It is known for its ability to inhibit the reuptake of these key neurotransmitters, thus enhancing their availability in the synaptic cleft. This compound is primarily utilized in research to study the mechanisms of mood disorders, depression, and other neurological conditions, making it a valuable tool for neuroscientific investigations. -
VMAT2 Inhibitor
(2S,3S,11bR)-Dihydrotetrabenazine is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2), exhibiting a Ki value of 593 nM. This compound disrupts the vesicular transport of monoamine neurotransmitters, including dopamine and serotonin, leading to decreased synaptic release of these neurotransmitters. (2S,3S,11bR)-Dihydrotetrabenazine is valuable for research into Huntington's chorea and other hyperkinetic disorders, providing insights into potential therapeutic strategies. -
VMAT2 Inhibitor
VMAT2-IN-4 is a selective inhibitor of the vesicular monoamine transporter-2 (VMAT2), demonstrating an affinity with a Ki value of 560 nM for [3H]-DTBZ binding and a more potent inhibition of [3H]-DA uptake into vesicles at a Ki of 45 nM. This compound effectively disrupts monoamine neurotransmitter packaging within vesicles, making it a valuable tool for investigating the mechanisms underlying methamphetamine addiction. VMAT2-IN-4 supports research into the modulation of dopaminergic signaling and its implications in addiction studies. -
VMAT2 Inhibitor
GZ-11608 is a potent and selective inhibitor of the vesicular monoamine transporter-2 (VMAT2) with a high affinity (Ki = 25 nM). This compound effectively reduces methamphetamine-induced dopamine release from isolated synaptic vesicles of dopaminergic neurons. Furthermore, GZ-11608 demonstrates rapid penetration into the brain and is characterized by an absence of neurotoxicity. It is a valuable tool for studying methamphetamine use disorder in therapeutic research. -
MCT4 Inhibitor
VB124 is a potent and selective inhibitor of monocarboxylate transporter 4 (MCT4), demonstrating significant activity with IC50 values of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 exhibits high selectivity for MCT4, distinguishing it from MCT1. This compound is valuable for research in areas such as cardiac hypertrophy, heart failure, and metabolic studies. -
MCT1/MCT4 Dual Inhibitor
Syrosingopine is a dual inhibitor of lactate transporters MCT1 and MCT4, effectively reducing glycolytic metabolism in cancer cells when combined with metformin. This compound has been shown to induce synthetic lethality, making it a valuable tool for cancer research. Additionally, Syrosingopine exhibits anti-hypertensive properties by depleting peripheral norepinephrine stores, presenting further avenues for cardiovascular studies. -
MCT4 Inhibitor
AZD0095 is a selective, orally bioavailable inhibitor of monocarboxylate transporter 4 (MCT4), characterized by an IC50 of 1.3 nM. This compound demonstrates significant antitumor activity by effectively inhibiting tumor growth in NCI-H358 xenograft models, particularly in combination with Cediranib. AZD0095 serves as a valuable tool for research into metabolic modulation and therapeutic strategies in cancer biology. -
MCT4 Inhibitor
MSC-4381 is a selective inhibitor of monocarboxylate transporter 4 (MCT4/SLC16A3), exhibiting an IC50 of 77 nM and a Ki of 11 nM. This compound effectively inhibits lactate efflux and decreases cellular viability in cells with high MCT4 expression. MSC-4381 serves as a valuable tool for research involving MCT4 transporter inhibition and features a reactive alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
MCT Inhibitor
MCT-IN-1 is a potent inhibitor of monocarboxylate transporters (MCT1 and MCT4), exhibiting IC50 values of 9 nM and 14 nM, respectively. This compound is particularly relevant for research into solid tumors, offering valuable insights into metabolic modulation and therapeutic strategies targeting tumor microenvironments. MCT-IN-1 serves as a crucial tool for investigating the role of lactate transport in cancer cell proliferation and survival. -
PepT1/MCT1 Inhibitor
N-Acetyl-R-leucine is an N-substituted chiral amino acid that functions as an inhibitor of the peptides transporter PepT1 and the monocarboxylate transporter MCT1, with IC50 values of 0.74 mM and 11 mM, respectively. This compound is valuable for investigating transporter activity and can be utilized in LysoTracker signaling studies, contributing to research on cellular metabolism and related pathways. -
MCT1 Inhibitor
MCT1-IN-2 is a potent inhibitor of monocarboxylate transporter 1 (MCT1), which plays a key role in cellular metabolism by facilitating the transport of lactate and other monocarboxylates. This compound has demonstrated significant anti-cancer activity, making it a valuable tool for research in cancer metabolism and therapeutic development. MCT1-IN-2 is suitable for studies investigating the role of MCT1 in tumor growth and progression, as well as potential combination therapies targeting metabolic pathways in cancer cells. -
MCT1 Inhibitor
MCT1-IN-3 is a potent inhibitor of the monocarboxylate transporter 1 (MCT1), exhibiting an IC50 value of 81.0 nM. Additionally, this compound shows significant inhibitory activity against the multidrug transporter ABCB1. MCT1-IN-3 is valuable for research applications focused on cancer, particularly in elucidating the role of MCT1 in tumor metabolism and drug resistance. -
MCT Inhibitor
AR-C141990 hydrochloride is a selective inhibitor of monocarboxylate transporters (MCTs), specifically demonstrating pKi values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. This compound exhibits immunosuppressive properties and is utilized in research concerning graft versus host disease and metabolic regulation. Its ability to modulate lactate transport makes it a valuable tool for studying the role of MCTs in various biological processes.
