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Catalog No.
Product Name
Application
Product Information
Citations
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KCC2 inhibitor
VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). -
gastric H+/K+-ATPase inhibitor
Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro. -
Calcium Channel Inhibitor
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. -
IBAT inhibitor
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ?? 0.17 nM, 0.13 ?? 0.03 nM, and 5.8 ?? 1.6 nM for human IBAT, mouse IBAT, and canine IBAT. -
nuclear export receptor CRM1 inhibitor
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
calcium channel inhibitor
Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM). -
P-glycoprotein inhibitor
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. -
Serotonin reuptake inhibitor (SSRI)
Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. -
H+/K+-ATPase inhibitor
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1??0.4 μM. -
HCN channels inhibitor
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 ?M. -
TRPP3 channel inhibitor
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis. -
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. -
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. -
COX-1/COX-2 inhibitor
Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis. -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
HIV-1 protease/PTP1B inhibitor
Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases. -
PKA inhibitor
HA-1004 is a selective and multifunctional inhibitor of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and cyclic GMP-dependent protein kinase (PKG). It regulates key second messenger pathways involving cyclic AMP and cyclic GMP and has broad pharmacological effects. HA-1004 inhibits lipolysis and induces vascular smooth muscle relaxation, acting as a vasodilator. It also functions as a calcium antagonist, contributing to its ability to suppress contraction in rabbit aortic strips. In neurological models, HA-1004 has been shown to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models, suggesting potential relevance in addiction and neurochemical regulation. Its diverse actions make it a valuable tool for studying cardiovascular, metabolic, and neurobiological processes.
