Catalog No.
Product Name
Application
Product Information
Citations
-
pan HDAC inhibitor
Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity. -
Autophagy Inducer
Loperamide hydrochloride is an opioid receptor agonist that functions primarily as an autophagy inducer. This compound selectively inhibits human intestinal carboxylesterases (hiCE), contributing to its anti-diarrheal properties. Its unique mechanism of action makes Loperamide hydrochloride a valuable reagent for studies related to gastrointestinal motility and autophagy modulation in various biological contexts. -
Benzodiazepine Receptor Partial Agonist
Miltirone is a partial agonist of the central benzodiazepine receptor, exhibiting an IC50 value of 0.3 μM. This natural compound, derived from the root of Salvia miltiorrhiza, demonstrates significant biological activity by inducing ROS- and p53-dependent apoptosis. Additionally, Miltirone effectively inhibits carboxylesterase 2 (CES2) with a Ki of 0.04 μM and the main protease (Mpro) of SARS-CoV, making it valuable for research involving apoptosis, enzymatic regulation, and virology. -
hCE1 Inhibitor
Nevadensin is a selective inhibitor of human carboxylesterase 1 (hCE1), exhibiting an IC50 value of 2.64 μM, while demonstrating significantly lower selectivity for hCE2 (IC50 of 132.8 μM). This natural flavonoid has been shown to induce apoptosis and DNA damage in cancer cells, indicating its potential for therapeutic applications in oncology. Additionally, Nevadensin displays a range of bioactivities, including anti-inflammatory, anti-tumor, anti-hypertensive, anti-tubercular, antitussive, antioxidant, and anti-microbial effects, making it a valuable agent for various research investigations. -
Anti-cancer Agent
Dihydromethysticin is a naturally occurring compound primarily targeting carboxylesterase 1 and CYP2A5. This orally active agent has demonstrated the ability to upregulate NLRC3 and induce apoptosis, showcasing its potential as an anti-cancer agent. Research indicates that dihydromethysticin exhibits significant anticancer activity against colorectal cancer and lung adenoma, making it a valuable tool in cancer research and therapeutic development. -
Photosensitizer
Benz-AP is a potent photosensitizer that generates singlet oxygen, exhibiting a negative correlation with human carboxylesterase 2 (hCES2) activity. This compound demonstrates enhanced photocytotoxicity in cancer cells, particularly in environments with low hCES2 levels. Upon two-photon excitation (TPE), Benz-AP produces reactive oxygen species (ROS), effectively inducing cell death in cancer cells and tumor spheroids, making it a valuable tool for cancer research applications. -
Red Fluorescent Probe
DDAO is a red fluorescent probe designed for near-infrared (NIR) applications, featuring tunable excitation wavelengths ranging from 600 to 650 nm and an emission wavelength of 656 nm. This compound is effective for the detection of various enzyme activities, including β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin, and esterases. DDAO is a valuable tool for biological research and enzyme activity assays, facilitating sensitive detection and analysis in diverse experimental settings. -
Fluorescent Dye
4-Methylumbelliferyl Decanoate is a fluorogenic substrate primarily utilized for monitoring the hydrolytic activity of carboxylesterases. When cleaved by these enzymes, it emits fluorescence, facilitating the detection and quantification of enzyme activity in biological samples. This reagent is instrumental in studies involving drug metabolism, enzyme kinetics, and the functional characterization of esterases in various biological systems. -
Fluorochrome
DDAO phosphate diammonium is a fluorescent phosphatase substrate that serves as a sensitive probe for enzyme activity. With tunable excitation wavelengths ranging from 600 to 650 nm and a long emission wavelength of 656 nm, it facilitates the detection of various enzymes including β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin, and esterase. This reagent is ideal for applications in enzymology and biochemistry research, enabling real-time monitoring of enzyme activities in different biological systems. -
Carboxylesterase Substrate, Mitochondria Targeting Agent
CEMT is a selective substrate for carboxylesterases, functioning as a ratiometric two-photon fluorescent reporter probe. Upon hydrolysis by carboxylesterases, CEMT generates HMT, which facilitates mitochondrial pH sensing through ratiometric fluorescence changes in response to pH fluctuations. This compound specifically targets and covalently binds to mitochondria, minimizing leakage during acidification, thereby enabling in situ imaging of mitochondrial dynamics and pH variations within biological systems. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-3 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum plays a critical role as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters necessary for Wnt activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the modulation of Wnt signaling pathways. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-2 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum functions as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters, which are essential for Wnt activity. This compound is valuable for investigating the role of Notum in cancer biology and the modulation of Wnt signaling pathways. -
Carboxylesterase Inhibitor
WZU-13 is a potent inhibitor of carboxylesterase (CES), demonstrating significant inhibition of 77% at a concentration of 100 μM. This compound is valuable for research applications aimed at studying the role of CES in drug metabolism and detoxification processes. WZU-13 can aid in elucidating the enzymatic mechanisms and biological functions of CES in various physiological and pathological contexts. -
Precursor Form
Oseltamivir acid methyl ester hydrochloride is a precursor to the neuraminidase inhibitor oseltamivir acid, which exhibits antiviral activity against influenza viruses. Upon administration, it is metabolized by carboxylesterase 1 (CES1) to yield oseltamivir acid, facilitating its therapeutic effects. This reagent is primarily utilized in research applications focused on antiviral drug development and metabolic studies involving oseltamivir. -
Precursor Form
Oseltamivir acid methyl ester is a precursor of the neuraminidase inhibitor and antiviral agent oseltamivir acid. It is converted into oseltamivir acid by the enzyme carboxylesterase 1 (CES1). This compound is useful in research applications focused on antiviral therapeutic development and the mechanistic understanding of flu virus inhibition. -
Carboxylesterase
Esterase, pig liver is a type of carboxylesterase known for its role in the hydrolysis of a wide range of endogenous and exogenous substrates. This enzyme catalyzes the breakdown of carboxylic acid esters into corresponding alcohols and carboxylic acids, facilitating important biochemical reactions. Its extensive distribution in mammalian liver makes it a valuable tool in biochemical research, particularly for studies involving ester metabolism and enzyme kinetics. -
Aldicarb Metabolite
Aldicarb sulfoxide is a metabolite of aldicarb that primarily interacts with glutathione-linked enzymes in CHO-K1 cells. This compound exhibits inhibitory activity against cholinesterase (ChE) and carboxylesterase (CaE), with an IC50 of 10 μM in zebrafish models. Its mechanism of action and biological activity make it a valuable tool for research on neurotoxicology and enzymatic regulation. -
CES Inhibitor
Dibromsalicil is a selective inhibitor of carboxylesterases (CES), exhibiting inhibitory activity with IC50 values of 72.7 nM against human intestinal carboxylesterase (hiCE) and 53.5 nM against rabbit liver carboxylesterase (rCE). This compound demonstrates minimal activity against human liver carboxylesterase (hCE1) and cholinesterase, making it a valuable tool for research applications focused on drug metabolism and enzymatic activity modulation. Its specificity for hiCE and rCE positions Dibromsalicil as an important reagent for studying carboxylesterase-related pathways. -
Carrot Carboxylesterase Substrate
Tripropionin, a triglyceride, acts as a substrate for carrot carboxylesterase. It exhibits key biological activity as a hydrolyzable ester, making it suitable for applications in lipid nanoemulsion formulation. This compound can effectively serve as the oil phase for creating high-performance lipid nanoemulsion droplets, facilitating the encapsulation, stable storage, and controlled release of bioactive compounds such as Combretastatin A4. -
hCES2A Inhibitor
Isolicoflavonol is a potent inhibitor of hCES2A (Human carboxylesterase 2), exhibiting reversible and mixed inhibition of fluorescein diacetate hydrolysis. With Ki values below 1.0 μM, it serves as a valuable tool for exploring enzymatic activity and regulation in biochemical research. Its specificity and efficacy make it suitable for investigations into drug metabolism and enzyme kinetics. -
hCES2 Inhibitor
CES2-IN-1 is a reversible and selective inhibitor of human carboxylesterase 2 (hCES2), exhibiting an IC50 value of 6.72 μM. This compound effectively reduces CES2 levels in living cells, making it useful for studies involving drug metabolism. CES2-IN-1 has demonstrated efficacy in preclinical models for conditions such as irinotecan-induced delayed diarrhea and dextran sulfate sodium (DSS)-induced ulcerative colitis, supporting its application in gastrointestinal research. -
Synthetic Reagent
Ethyl phenylglyoxylate, an ethyl ester of phenylglyoxylic acid, serves as a synthetic reagent in chemical research. It is recognized as a potent inhibitor of chicken liver carboxylesterase, despite being a suboptimal substrate. Additionally, Ethyl phenylglyoxylate exhibits photoreactivity, enabling its excited triplet carbonyl to initiate various reactions, including intermolecular hydrogen abstraction, radical coupling, and cross-linking. This compound is valuable for studies involving enzyme inhibition and radical-mediated processes. -
Carboxylesterase Inhibitor
Tanshinone IIA anhydride is a potent irreversible inhibitor of human carboxylesterases, demonstrating Ki values of 1.9 nM for human carboxylesterase 1 and 1.4 nM for human intestinal carboxylesterase. This compound is valuable for studying the regulatory mechanisms of esterases in various biological processes. Its application extends to biochemical studies focused on enzyme inhibition and metabolic pathway analysis. -
CE Inhibitor
1-Methylisatin is a selective carboxylesterase (CE) inhibitor, exhibiting inhibitory constants of 38.2 μM for human isoform CE (hiCE) and 5.38 μM for human carboxylesterase 1 (hCE1). This compound interacts with human adult hemoglobin through hydrophobic binding and electrostatic interactions. 1-Methylisatin serves as a valuable tool for investigating the regulation of drug metabolism and biochemical pathways in vivo. -
PL/hCES1A Inhibitor
Pancreatic lipase/Carboxylesterase 1-IN-1 is a potent inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A), displaying IC50 values of 2.13 µM and 0.055 µM, respectively. This dual inhibition makes it a valuable tool for studying lipid metabolism and the enzymatic pathways related to drug metabolism and detoxification processes. It has potential applications in research focused on obesity, metabolic disorders, and pharmacokinetics. -
hCES2A Inhibitor
Gancaonin I is an isoflavone that serves as a moderate inhibitor of human carboxylesterase 2 (hCES2A) with an IC50 of 1.72 μM. It effectively inhibits the hCES2A-mediated hydrolysis of fluorescein diacetate (FD), making it a valuable tool for research applications involving enzyme regulation and drug metabolism studies. -
Carboxylesterase (CES) Inhibitor
PMPMEase-IN-1 is a selective inhibitor of carboxylesterase (CES) that targets PMPMEase activity, thereby modulating protein methylation processes. This compound demonstrates potential anti-cancer activity by enhancing sensitivity to polyisoprenyl derivatives, with an effective concentration (EC50) observed in inducing degeneration of human neuroblastoma SH-SY5Y cells. By specifically inhibiting PMPMEase, PMPMEase-IN-1 may contribute to the regulation of polyisoprenyl protein metabolism, promoting normal cellular function. Its utility in research could pave the way for therapeutic advancements in treating cancer and degenerative diseases. -
hCES2A Inhibitor
CES2A-IN-3 is a potent inhibitor of human carboxylesterase 2A (hCES2A), acting through a serine-targeting covalent mechanism with an IC50 of 0.12 nM. This compound holds significant promise for research applications related to gastrointestinal disorders, including diarrhea and ulcerative colitis, by modulating enzyme activity linked to these conditions. Its high specificity and efficacy make it an essential tool for exploring hCES2A's role in related biological pathways. -
Flavonoids Compound
Kushenol X is a flavonoid compound derived from the roots of Sophora flavescens, known for its inhibition of β-glucuronidase and human carboxylesterase 2 (hCE2). With IC50 values of 2.07 μM and 3.05 μM respectively, it serves as a valuable tool for studying enzymatic pathways and their roles in pharmacokinetics. This compound is relevant for research in drug metabolism and therapeutic interventions involving glycosylated and esterified compounds. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-4 is a highly potent inhibitor of carboxylesterase, exhibiting an IC50 of 1.58 nM. This compound facilitates research into cholesterolemia by effectively modulating carboxylesterase activity, making it a valuable tool in the study of lipid metabolism and associated disorders. -
Stable Isotope
Ethyl phenylglyoxylate-d5 is a deuterium-labeled derivative of Ethyl phenylglyoxylate, primarily functioning as a stable isotope for chemical research. This compound serves as a synthetic reagent and is recognized as a potent inhibitor of chicken liver carboxylesterase, despite being a poor substrate. Additionally, Ethyl phenylglyoxylate-d5 demonstrates photoreactivity; its excited triplet carbonyl can facilitate intermolecular hydrogen abstraction, radical coupling, and cross-linking reactions, making it valuable in various biochemical studies and synthetic applications. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-5 is an irreversible and competitive inhibitor of carboxylesterase with an IC50 of 21.7 nM for porcine liver carboxylesterase. This reagent is suitable for studies investigating the role of carboxylesterases in metabolic processes and is particularly relevant for research pertaining to hypocholesterolemia. Its specificity and potency make it a valuable tool in biochemical and pharmacological investigations. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-1 is a potent carboxylesterase inhibitor, demonstrating significant inhibitory activity at a concentration of 50 μg/mL. By interfering with carboxylesterase function, it serves as a valuable tool in the study of enzyme regulation and pesticide effects on biological systems. This compound is suitable for research applications focusing on enzyme inhibition and the molecular mechanisms of pesticide action. -
Carboxylesterase (CES) Inhibitor
SQ-24798 is a potent inhibitor of carboxylesterase (CES), specifically designed to bind the zinc ion in the enzyme's active site via its sulfhydryl group, leading to effective enzyme inhibition. This compound exhibits high affinity and specificity, making it a valuable tool in biochemical research focused on understanding CES-related pathways. Its applications include studying drug metabolism and the physiological roles of CES in various biological processes. -
AChE/CES Inhibitor
Heptenophos is a potent inhibitor of acetylcholinesterase (AChE) and plasma carboxylesterase (CES). By obstructing AChE activity, Heptenophos leads to the accumulation of acetylcholine at cholinergic synapses, which can result in symptoms characteristic of organophosphate poisoning. Its rapid toxicity in animal models, such as male albino mice, allows for the investigation of detoxification strategies, particularly in conjunction with agents like obidoxime and Memantine. This compound is widely utilized in research exploring the mechanisms underlying organophosphate effects and potential antidotal treatments. -
Carboxylesterase Substrate
Dibutyl malate serves as a substrate for carboxylesterase, an enzyme critical in the hydrolysis of ester bonds. This compound is particularly useful in biochemical studies investigating enzymatic activity and substrate specificity. It is also applicable in drug metabolism and pharmacokinetic research, aiding in the understanding of ester-containing pharmaceuticals. -
Chelating Agent, Mitochondrial Electron Transport Chain Inhibitor, Carboxylesterase Inhibitor
2-Thenoyltrifluoroacetone is a chelating agent that targets the mitochondrial electron transport chain, exhibiting an IC50 value of 51.5 μM. It effectively chelates various metal ions and demonstrates cytotoxicity along with anti-tumor activity. This compound holds potential for applications in the treatment of diseases linked to mitochondrial dysfunction, contributing valuable insights into related therapeutic strategies. -
BuChE inhibitor
Iso-OMPA (Tetraisopropyl pyrophosphoramide) is a selective inhibitor of butyrylcholinesterase (BuChE), functioning through irreversible inhibition. This compound is primarily utilized in research to investigate the mechanisms of BuChE and the resulting effects on acetylcholine metabolism. Iso-OMPA has been shown to enhance soman toxicity in rat models, linked to the inhibition of plasma carboxylesterase (CarbE), making it a valuable tool in studies of nerve agent effects and cholinergic signaling. -
Detection Substrate
3-Indoxyl butyrate serves as a chromogenic substrate for carboxylesterase (CES), leading to the generation of a blue precipitate upon enzymatic cleavage. This reaction makes it a valuable tool for detecting and quantifying CES activity in biological samples. Its sensitivity and specificity enhance research applications in enzyme kinetics and drug metabolism studies. -
Aldicarb Metabolite
Aldicarb sulfoxide-d3 is a deuterium-labeled metabolite of Aldicarb that serves as a valuable tool in chemical research. This compound primarily targets glutathione-linked enzymes, demonstrating significant inhibitory effects on cholinesterase (ChE) and carboxylesterase (CaE) pathways, with IC50 values of 10 μM in zebrafish models. Its utility extends to studies on metabolic pathways and enzyme interactions, contributing to a deeper understanding of neuroactive compounds and their biological implications.
