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Catalog No.
Product Name
Application
Product Information
Citations
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Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies. -
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. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
DPP4 Inhibitor
Sitagliptin hydrochloride is a selective DPP4 inhibitor, demonstrating an IC50 of 19 nM. By inhibiting DPP4, this compound prevents the breakdown of incretin hormones, such as GLP-1 and GIP, ultimately increasing their active levels. Additionally, sitagliptin can stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, independent of DPP-4 inhibition. This reagent is applicable in research involving type 1 and type 2 diabetes, and it also exhibits protective effects on pancreatic islet grafts in type 1 diabetes models. -
ICMT Inhibitor
POP-3MB is an inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 2.5 μM. It effectively alters the subcellular localization of K-Ras, leading to inhibition of Ras activation. Additionally, POP-3MB demonstrates the capacity to inhibit Erk phosphorylation, making it a valuable tool for research into Ras signaling pathways and related oncogenic processes. -
S1P2 Receptor Inhibitor
S118 is an orally active inhibitor of the sphingosine-1-phosphate receptor 2 (S1P2 receptor), which blocks the binding of Dpr1, subsequently reducing β-catenin accumulation. This mechanism inhibits nuclear translocation of the S1P2 receptor, contributing to the attenuation of inflammation, fibrosis, and epithelial-mesenchymal transition (EMT). S118 demonstrates potential for use in research related to idiopathic pulmonary fibrosis (IPF) and other fibrotic diseases. -
Platelet Aggregation Inhibitor
12(S)-HETrE is a fatty acid metabolite that serves as a potent inhibitor of platelet aggregation. This compound demonstrates significant biological activity in modulating thrombus formation and is valuable in thrombosis-related research applications. Researchers can utilize 12(S)-HETrE to study the molecular mechanisms underlying platelet function and explore potential therapeutic targets in cardiovascular diseases. -
PTP4A3 Inhibitor
JMS-053 is a potent and reversible inhibitor of PTP4A3, with an IC50 value of 18 nM. This compound also exhibits significant inhibitory activity against PTP4A1 and PTP4A2, with IC50s of 50 nM and 53 nM, respectively. Additionally, JMS-053 demonstrates inhibition of CDC25B and DUSP3 with IC50 values of 92.6 nM and 207.6 nM, respectively. Through mechanisms such as interference with RhoA and STAT3/p38 signaling pathways, JMS-053 effectively suppresses tumor cell proliferation and migration, making it a valuable tool for investigating various cancers, including ovarian, breast, and colon cancer. -
CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
S1P Inhibitor
Pro-FTY is a sphingosine-1-phosphate (S1P) inhibitor functioning as an anticancer prodrug derived from FTY720. It selectively disrupts S1P signaling in cancer cells using a drug delivery system that reacts with acrolein, demonstrating significant cytotoxic effects on breast cancer cells, including multidrug-resistant variants. Pro-FTY effectively suppresses tumor growth in xenograft models with 4T1 cells and organoids, while maintaining immune cell integrity by avoiding lymphocytopenia. This reagent is valuable for research in cancer therapy and resistance mechanisms. -
Histamine receptors inhibitor
Histamine Receptors Inhibitor 1 (compound 303) functions as an inhibitor of H1 and H4 histamine receptors. This compound demonstrates key biological activity in modulating inflammatory processes and is particularly relevant for research applications focusing on autoimmune, allergic, and ocular conditions. Its ability to selectively inhibit these receptors makes it a valuable tool for investigating histamine-mediated pathways in various biological contexts. -
PDD4 Inhibitor
Sitagliptin phosphate is a selective DPP4 inhibitor with a powerful mechanism of action, featuring an IC50 value of 19 nM. By inhibiting DPP4, this compound prevents the degradation of incretins such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), resulting in enhanced active incretin levels. Additionally, it can directly stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, which operates independently of DPP-4. Sitagliptin phosphate is valuable for researching both type 1 and type 2 diabetes and demonstrates protective effects on pancreatic islet grafts in type 1 diabetes models. -
Platelet Aggregation Inhibitor
Notoginsenoside Fc is a protopanaxadiol-type saponin derived from the leaves of Panax notoginseng, functioning primarily as a platelet aggregation inhibitor. This compound effectively mitigates platelet aggregation and has been shown to enhance reendothelialization after vascular injury in diabetic rat models by promoting autophagy. Its biological activity makes Notoginsenoside Fc a valuable reagent for research in cardiovascular health and vascular regeneration. -
Histamine Inhibitor
Spinacetin is a natural compound derived from Inula japonica that acts as a histamine inhibitor. It effectively inhibits histamine release, demonstrating notable anti-inflammatory properties. This reagent is valuable for research applications focused on allergic responses, inflammation studies, and the elucidation of histamine-related pathways. -
Histamine Receptor Inhibitor
Quinotolast sodium is a histamine receptor inhibitor that effectively blocks the release of histamine, LTC4, and PGD2 in a concentration-dependent manner within the range of 1-100 μg/mL. This compound is valuable for research applications focused on allergic responses and inflammatory processes, as it helps elucidate the mechanisms of histamine signaling and associated pathophysiologies. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
Platelet Aggregation Inhibitor
2'-Hydroxyflavanone is a flavanone that functions as a platelet aggregation inhibitor. It demonstrates significant bioactivity by inhibiting platelet aggregation induced by arachidonic acid and adenosine diphosphate, with IC50 values of 47.8 μM and 147.2 μM, respectively. Additionally, 2'-hydroxyflavanone has been implicated in inhibiting cancer cell proliferation and inducing apoptosis, making it valuable for research in cancer and inflammatory pathways. -
Noradrenergic Reuptake Inhibitor
Maprotiline is a selective noradrenergic reuptake inhibitor that exhibits significant antidepressant activity and also shows promise in antitumor and neuropathic pain relief. It facilitates cancer cell apoptosis through modulation of the ERK signaling pathway and interaction with cellular retinoic acid-binding protein 1 (CRABP1). This compound is valuable for research in mental health disorders, oncology, and pain management. -
LPAAT-β Inhibitor
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β), showing significant inhibition of tumor cell growth. It exhibits IC50 values in the range of 0.1-0.8 μM across various leukemia cell lines and effectively induces caspase activation in DHL-4 and Ramos cells. In combination with Rituximab, CT 32228 promotes apoptosis and demonstrates a 50% growth delay in xenograft models. This reagent is suitable for research applications targeting acute leukemia. -
Platelet Aggregation Inhibitor
Ergosta-7,22-dien-3-one functions as a platelet aggregation inhibitor, derived from the fruiting bodies of Ganoderma lucidum. This compound is known to enhance nitric oxide production and promote the expression of specific genes alongside the synthesis of Toll-like receptors (TLRs), cytokines, chemokines, and cellular adhesion molecules in vitro. Ergosta-7,22-dien-3-one is valuable for research in hematology, inflammation, and cellular signaling pathways. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a selective inhibitor of the cannabinoid CB1 receptor. This neurosteroid, a key precursor in steroid hormone synthesis, can mitigate the effects of tetrahydrocannabinol (THC) by blocking its action at CB1 receptors. Additionally, Pregnenolone monosulfate sodium serves as a TRPM3 channel activator and has been shown to weakly activate TRPM1 channels. Its unique properties make it a valuable tool for investigating cannabinoid signaling and neuroprotective strategies against cannabis-related effects. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a selective inhibitor of the cannabinoid CB1 receptor. By inhibiting the effects of tetrahydrocannabinol (THC) mediated through the CB1 receptors, it offers potential neuroprotective properties against cannabis intoxication. Additionally, Pregnenolone monosulfate serves as a TRPM3 channel activator and exhibits weak activation of TRPM1 channels, making it valuable for research in neuropharmacology and cannabinoid signaling pathways. -
Icmt Inhibitor
Cysmethynil is an inhibitor of Isoprenylcysteine carboxylmethyltransferase (Icmt) with an IC50 of 2.4 μM. It disrupts RAS membrane binding and interferes with EGF signal transduction, leading to cell cycle arrest in the G1 phase and the induction of autophagy. Cysmethynil effectively inhibits the proliferation of PC3 prostate cancer cells and demonstrates synergistic effects with chemotherapeutic agents such as Paclitaxel and Doxorubicin. This compound is applicable for research into solid tumors, including prostate cancer. -
Platelet Aggregation Inhibitor
5(S),15(S)-DiHETE is a platelet aggregation inhibitor that functions as an activated intermediate in the biosynthesis of specialized pro-resolving mediators. With an IC50 of 1.3 μM, it effectively reduces platelet aggregation. Additionally, 5(S),15(S)-DiHETE enhances the rate of biosynthesis for lipoxins A4 (LXA4) and B4 (LXB4), making it valuable for research applications in inflammation and resolution processes. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
Histamine-release Inhibitor
Panaxydiol is a histamine-release inhibitor that effectively suppresses histamine secretion in biological systems. This compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the formation of diverse chemical linkages. Its unique properties make Panaxydiol a valuable reagent for researchers involved in chemical biology, drug discovery, and the development of innovative therapeutic strategies. -
Histamine Receptor Inhibitor
AM-0466 is a selective histamine receptor inhibitor primarily targeting voltage-gated sodium channel NaV1.7. This compound demonstrates potent anti-pruritic activity in histamine-induced itch models and exerts significant analgesic effects in capsaicin-induced pain assays. Its optimized pharmacokinetic profile supports its use in advanced in vivo research for evaluating efficacy in pain modulation and itch relief. -
Histamine Receptor Inhibitor
Fenethazine is a histamine receptor inhibitor known for its antihistamine activity. It effectively alleviates allergic reactions and related symptoms. Additionally, its structural congeners exhibit anticholinergic effects, making fenethazine a candidate for research into therapeutic interventions for Parkinson's disease. This compound is valuable for studies focused on histaminergic pathways and associated disorders. -
Histamine H3 Receptor Antagonist/Serotonin Transporter Inhibitor
JNJ-28583867 is a selective histamine H3 receptor antagonist with a Ki of 10.6 nM and an inhibitor of the serotonin transporter (SERT) with a Ki of 3.7 nM. This compound shows promise in modulating neurotransmitter systems and can be utilized in research focusing on depression and related neuropsychiatric disorders. Its unique mechanism makes it a valuable tool for studying the interplay between histaminergic and serotonergic pathways. -
Histamine Receptor Inhibitor
(R)-Azelastine hydrochloride is a histamine receptor inhibitor that effectively down-regulates the expression of H1, M1, and M3 receptors. This compound exhibits notable biological activity by inhibiting the proliferation of human nasal epithelial cells (HNEpC). Its applications in research include studying allergic reactions and evaluating the roles of histamine receptors in various cellular processes. -
Histamine Receptor Inhibitor
Linadryl is a histamine receptor inhibitor that exhibits antihistaminic properties. It demonstrates a moderate impact on gastric acid secretion following oral administration, approximately half that of Diphenhydramine. Linadryl is primarily utilized in research focusing on allergic responses, gastrointestinal function, and exploring the broader effects of histamine modulation in various biological systems. -
Histamine H1 Receptor Inhibitor
SUN-1334H free base is a potent orally active inhibitor of the histamine H1 receptor, demonstrating an IC50 of 20.3 nM and a Ki value of 9.7 nM. This compound effectively inhibits histamine-induced contractions in isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base has significant applications in research related to bronchoconstriction, allergic responses, and rhinitis, as evident in its ability to mitigate histamine-induced bronchoconstriction in guinea pigs, skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride is a potent inhibitor of phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. Additionally, it acts as an antagonist of the H1-histamine receptor, contributing to its anti-inflammatory properties. Fenspiride is primarily utilized in research related to respiratory diseases, offering insights into mechanisms of action and potential therapeutic applications. -
Histamine Receptor Inhibitor
VUF14738 is a bidirectional photoswitch antagonist targeting the histamine H3 receptor. This compound exhibits rapid and reversible photoisomerization, allowing for modulation of binding affinity in response to illumination. Its unique properties make VUF14738 ideal for real-time electrophysiological studies, facilitating research into the dynamic light modulation of receptor activation and the underlying mechanisms of histamine signaling. -
EBOV/MARV Inhibitor
CP19 is a histamine receptor antagonist that functions as an entry inhibitor for both Ebolavirus (EBOV) and Marburgvirus (MARV), demonstrating IC50 values of 3.4 μM and 29.5 μM, respectively. With selectivity index (SI) values of 29.4 for EBOV and 3.4 for MARV, CP19 exhibits notable antiviral activity. This compound is valuable for research into viral entry mechanisms and the development of antiviral strategies targeting EBOV and MARV. -
Histamine Receptor Inhibitor
Mequitamium iodide is a potent histamine receptor inhibitor, demonstrating significant antiallergic and bronchodilatory properties. It effectively antagonizes airway contraction and inflammatory responses triggered by histamine and various antigens, exhibiting nanomolar affinity for H1 and smooth muscle receptors. When delivered via aerosol, Mequitamium iodide markedly reduces histamine- and antigen-induced airway pressure increases in allergic mouse models. Additionally, it decreases eosinophil accumulation in the airways and inhibits platelet aggregation and bronchoconstriction induced by PAF. This compound is valuable for investigating allergic diseases, including rhinitis and asthma. -
Histamine Receptor Inhibitor
Impentamine dihydrobromide is a histamine H3 receptor antagonist known for its potent antihistamine activity. This compound demonstrates selective H3 antagonism, with a pA2 value of 8.4, indicating significant efficacy in guinea pig jejunum studies. Impentamine dihydrobromide binds specifically to the H3 receptor, making it valuable for research in neuropharmacology and related fields investigating histamine's role in neurotransmission and various physiological processes. -
Gastric Secretory Inhibitor
UK-9040 is an orally active inhibitor of gastric secretion that targets histamine receptors. This compound effectively reduces gastric acid, pepsin, and volume output in response to food, insulin, histamine, N-methyl histamine, and pentagastrin. UK-9040 is valuable for research applications focused on gastric physiology and the modulation of acid secretion. -
Histamine Receptor Inhibitor
Hetramine is a histamine receptor inhibitor known for its antihistamine and antiallergic properties. It effectively prevents histamine-induced intestinal contractions and mitigates allergic responses, including anaphylactic shock, in animal models such as guinea pigs. This compound is useful in research related to allergy mechanisms and gastrointestinal function. -
Histamine H3 Antagonist/Serotonin Reuptake Inhibitor
Histamine H3 antagonist-1 is a potent histamine H3 receptor antagonist and serotonin reuptake inhibitor, playing a critical role in neuromodulation. Its primary biological activity makes it valuable for research in the field of depression and related neuropsychiatric disorders. This compound offers insights into the interactions between histamine and serotonin signaling pathways, facilitating the development of novel therapeutic strategies. -
Histamine Receptor Inhibitor
Perphenazine-d8 dihydrochloride is a deuterium-labeled derivative of Perphenazine, primarily functioning as a histamine receptor inhibitor. This compound exhibits potent antipsychotic properties by interacting with serotonin and dopamine receptors. It is valuable for research focused on neuropharmacology, chemical biology, and the study of receptor-ligand interactions in psychiatric disorders. -
Histamine Receptor Inhibitor
(R)-Azelastine is a histamine receptor inhibitor with notable antiallergic properties. This compound effectively downregulates the levels of H1R, M1R, and M3R, making it significant for research related to allergy and inflammation. Additionally, (R)-Azelastine has been demonstrated to inhibit the proliferation of human nasal epithelial cells (HNEpC), indicating its potential applications in studies of respiratory conditions and allergic responses. -
Histamine Release Inhibitor
Acreozast (TYB-2285) is a potent histamine release inhibitor that acts by blocking the release of histamine primed with interleukin-3 (IL-3). This compound has demonstrated the potential to modulate allergic inflammation in vivo through the suppression of inflammatory mediators. Acreozast is of particular interest for research applications involving allergy and immune response studies. -
Histamine Receptor Inhibitor
Azatadine is a histamine receptor inhibitor that functions by antagonizing H1 and H2 subtypes. This compound exhibits significant biological activity in blocking histamine-mediated processes, making it valuable in research related to allergic responses and motion sickness. Azatadine's mechanism of action also extends to cholinergic pathways, providing further insights into neuropharmacological studies. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders. -
Histamine Receptor Inhibitor
(S)-Azelastine is a selective antihistamine that primarily targets the histamine H1 receptor. This compound exhibits antiallergic and antiasthmatic properties, demonstrating the ability to downregulate levels of histamine receptors H1R, M1R, and M3R. Additionally, (S)-Azelastine has been found to inhibit the proliferation of human nasal epithelial cells, making it a valuable reagent for research in allergy and asthma mechanisms.
