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Catalog No.
Product Name
Application
Product Information
Citations
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NMDAR/TRPM4 inhibitor
Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury. -
HDAC inhibitor
HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models. -
Bone resorption inhibitor
Chicken calcitonin is a peptide hormone involved in the regulation of calcium metabolism. It inhibits bone resorption by suppressing the motility and activity of osteoclasts, as demonstrated in neonatal rat models. This hormone plays a key role in maintaining bone homeostasis and is of interest in bone-related research. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
Potassium Channel Inhibitor
Endoxifen Z-isomer hydrochloride is a selective potassium channel inhibitor that acts as a potent metabolite of Tamoxifen, exhibiting over 100-fold increased potency compared to its parent compound. This compound effectively inhibits PKCβ1 kinase activity, leading to decreased phosphorylation of AKT at Ser473 and its substrates, which ultimately promotes apoptosis. Endoxifen Z-isomer hydrochloride demonstrates significant anticancer effects, particularly against hormone-resistant metastatic breast cancer, making it a valuable reagent for cancer research applications. -
Na+/K+-ATPase Inhibitor
Cryptanoside A is a potent Na+/K+-ATPase inhibitor derived from the stems of Cryptolepis dubia. This cardiac glycoside epoxide exhibits significant cytotoxic effects against various cancer cell lines. Additionally, Cryptanoside A enhances the expression of Akt and the p65 subunit of NF-κB, making it a valuable tool for studying cancer biology and the regulatory pathways involved in cell survival and proliferation. -
Proton Pump Inhibitor
Revaprazan is a reversible proton pump inhibitor that targets gastric acid secretion. It provides protection to the gastric mucosa and inhibits the degradation of IkappaB-alpha, as well as the inactivation of Akt, leading to a reduction in H. pylori-induced COX-2 expression. This compound is valuable in research applications related to infection and inflammation, particularly in studies of H. pylori-infected gastric inflammation and gastric ulcer pathophysiology. -
TRPC6 Inhibitor
Larixyl acetate is a potent and selective inhibitor of the TRPC6 channel, exhibiting IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. This compound demonstrates significant biological activity by preventing human papillomavirus (HPV) infections and offers protective effects against systemic endothelial dysfunction induced by traumatic brain injury. Larixyl acetate is a valuable tool for research in cellular signaling and the therapeutic exploration of TRPC6-related pathologies. -
TRPM7 Inhibitor
TRPM7-IN-1 is a selective inhibitor of the TRPM7 ion channel, a critical regulator of cellular functions. This compound induces cell cycle arrest and apoptosis in cancer cell lines, such as MCF-7 and BGC-823, while also reducing cell migration. TRPM7-IN-1 modulates expression levels of key proteins, decreasing vimentin and increasing E-cadherin, and acts through the PI3K/Akt signaling pathway. Its ability to diminish TRPM7 expression and function positions TRPM7-IN-1 as a promising candidate for investigation in the context of breast and gastric cancer metastasis. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
Adenosine reuptake Inhibitor
KF24345 free base is an orally active inhibitor of adenosine uptake. It effectively inhibits adenosine uptake in erythrocytes from humans, mice, rabbits, and hamsters, demonstrating IC50 values of 59.5, 130.1, 104.2, and 30.9 nM, respectively. Additionally, KF24345 free base exhibits anti-inflammatory properties by inhibiting lipopolysaccharide (LPS)-induced production of TNF-α and preventing leukopenia in murine models, making it a valuable tool for research in inflammatory responses and adenosine signaling pathways. -
ASK1 Inhibitor
ASK1-IN-11 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of less than 200 nM. This compound also demonstrates inhibitory effects on TNF-α, MYLK/MLCK kinases, and hERG potassium channels. The primary research applications of ASK1-IN-11 include investigations into inflammation-related pathways. -
Chloride Channel Inhibitor
Shikonin is a potent inhibitor of the TMEM16A chloride channel, exhibiting an IC50 value of 6.5 μM. This compound functions as a specific inhibitor of pyruvate kinase M2 (PKM2) and also modulates inflammatory pathways by inhibiting TNF-α and NF-κB activation. In addition, Shikonin decreases exosome secretion by impairing glycolytic processes and effectively inhibits AIM2 inflammasome activation. Its diverse activities make it a valuable reagent for investigating cellular signaling and inflammatory responses in research applications. -
HIV-1 Entry Inhibitor
Trilobatin is a natural sweetener extracted from Lithocarpus polystachyus Rehd, functioning primarily as an HIV-1 entry inhibitor by targeting the HIV-1 Gp41 envelope protein. It demonstrates neuroprotective effects and acts as a selective SGLT1/2 inhibitor, promoting the proliferation of human hepatoblastoma cells. Trilobatin is valuable for research involving HIV-1 entry mechanisms and potential therapeutic applications in hepatoblastoma and neuroprotection studies. -
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. -
V-ATPase Inhibitor
Bafilomycin D is a specific inhibitor of vacuolar-type ATPase (V-ATPase), blocking proton translocation and disrupting acidic environments within cells. This compound exhibits significant antimicrobial, insecticidal, herbicidal, and cytotoxic activities, making it a valuable tool for biochemical research. It is useful in studies related to cellular metabolism, ion homeostasis, and the investigation of V-ATPase functions across various biological systems. -
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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Potassium Channel Inhibitor
Dequalinium Chloride is a selective inhibitor of potassium channels sensitive to Apamin. This cationic, lipophilic compound exhibits mitochondrial toxicity and additionally acts as an antagonist of the α7 nicotinic acetylcholine receptor. Dequalinium Chloride demonstrates broad-spectrum antimicrobial properties, exhibiting both bactericidal and fungicidal activities, making it valuable for research in cellular physiology and microbiology. -
Proton Pump Inhibitor
Pantoprazole sodium is a potent proton pump inhibitor that specifically targets the H+/K+-ATPase enzyme with an IC50 of 6.8 μM. This substituted benzimidazole effectively reduces gastric acid secretion, demonstrating significant anti-secretory and anti-ulcer activities. Additionally, studies indicate that Pantoprazole sodium can enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable tool in cancer research and gastrointestinal studies. -
Mdr1p Inhibitor
P-gp-IN-34 is a potent inhibitor of the Mdr1p pump, targeting multidrug resistance in various biological contexts. It has demonstrated efficacy in inhibiting the yeast-to-hyphal transition in Candida albicans, a critical process in its pathogenicity. This compound is suitable for research applications focused on candidiasis and the mechanisms of antifungal resistance. -
Pma1p-ATPase Inhibitor
ATPase-IN-5 is a potent inhibitor of Pma1p-ATPase, exhibiting an IC50 value of 12.7 μM. This compound is critically important in the study of antifungal mechanisms, providing insights into yeast cell metabolism and enzyme regulation. ATPase-IN-5 offers valuable applications in antifungal research, enabling the exploration of new therapeutic strategies. -
Sodium Channel Inhibitor
Lamotrigine-13C3 is a stable isotope-labeled derivative of Lamotrigine, a highly effective sodium channel inhibitor. This compound selectively targets voltage-gated Na+ channels, leading to stabilization of presynaptic neuronal membranes and a subsequent reduction in glutamate release. Lamotrigine-13C3 is suitable for research applications related to epilepsy, focal seizures, and other neurological disorders. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
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. -
TRPML1/3 Inhibitor
(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
