Carboxylesterase (CES)
Carboxylesterase; Carboxylic-ester Hydrolase
Cboxylesterases (CES) are serine hydrolases belonging to the superfamily of proteins with α/β hydrolase fold. Cboxylesterases are widely distributed in many tissues including liver, intestine, lung and kidney. Cboxylesterases catalyze the ester cleavage of a large number of structurally diverse ester- or amide-containing substrates into the corresponding alcohol and carboxylic acid. Actually, Cboxylesterases can hydrolyze ester, thioester, amide, and carbamate linkages in a wide variety of endo- and xenobiotic compounds, thus playing key roles in both endobiotic metabolism, and in activation and/or detoxification of xenobiotics. In humans, three Cboxylesterases have been identified, namely human carboxylesterase 1 (CES1), CES2, and CES3. Among them, CES1 and CES2 are two widely studied isoenzymes involved in xenobiotic metabolism. Cboxylesterases play an important role in the metabolism of various xenobiotics including ester drugs and environmental toxicants, and also participate in lipid homeostasis[1].
Carboxylesterase (CES) Isoform Specific Products
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Carboxylesterase (CES) Related Products (54)
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Carboxylesterase (CES) Isoform Comparison
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Bakuchiol
0 ImagesSynonyms: (S)-(+)-BakuchiolBakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.
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Miltirone
0 ImagesSynonyms: RosmariquinoneMiltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
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WWL113
0 ImagesWWL113 is a selective and orally active Ces3 and Ces1f inhibitor, with IC50 values of 120 nM and 100 nM for Ces3 and Ces1f, respectively. WWL113 appears to show excellent selectivity for the 60-kDa serine hydrolase (or hydrolases).
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DDAO
0 ImagesCat. No.: HY-114879CAS No.: 118290-05-4DDAO is a promising near-infrared (NIR) red fluorescent probewith tunable excitation wavelength (600-650nm) and longemission wavelength(λem=656nm). DDAO can de desiged for detection of the activities of different enzymes such asβ-galactosidase,sulfatase, proteinphosphatase2A,carboxylesterase 2, humanalbumin andesterases.
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WWL229
0 ImagesWWL229 is a selective inhibitor of carboxylesterase 3 (CES3) with an IC50 1.94 μM. WWL229 attenuates LPS (HY-D1056)-induced pro-inflammatory cytokine mRNA levels, inhibits lipolysis and adipose thermogenesis, impairs mitochondrial function, and promotes lipid storage. WWL229 can be used for the research of obesity, insulin resistance, type 2 diabetes, and lung inflammation.
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CEMT
0 ImagesCat. No.: HY-D3166CAS No.: 2413816-64-3CEMT is a carboxylesterase (CES) substrate and a ratiometric two-photon fluorescent reporter probe. CEMT can be hydrolyzed by CES to generate HMT, which is used for mitochondrial pH sensing. After activation by CES, CEMT exhibits ratiometric fluorescence changes in response to pH variations. CEMT targets and covalently binds to mitochondria, and can avoid leakage during acidification, thus enabling in situ imaging (Ex/Em = 410 nm/550 nm).
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CycLuc1 methyl ester
0 ImagesCat. No.: HY-D3461CAS No.: 2770784-56-8CycLuc1 methyl ester (Example 1) is a selective CES1 substrate and indirect bioluminescent inducer. CycLuc1 methyl ester undergoes catalytic hydrolysis via CES1-mediated ester bond cleavage to form a carboxyl product. The carboxyl product of CycLuc1 methyl ester undergoes an oxidation reaction with luciferase to generate a detectable bioluminescent signal. CycLuc1 methyl ester enables quantitative detection of CES1 activity.
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LP-935001
0 ImagesCat. No.: HY-182632CAS No.: 1875037-24-3LP-935001 is a Notum carboxylesterase inhibitor with an IC50 of 0.4 nM.LP-935001 prevents palmitoleate group removal from Wnt proteins, restores Wnt/β-catenin signaling.LP-935001 enhances cortical bone thickness in rodent models.LP-935001 can be used for the research of bone loss/nonvertebral fractures.
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Nevadensin
0 ImagesSynonyms: LysionotinNevadensin (Lysionotin), a natural flavonoid, is a selective human carboxylesterase 1 (hCE1) inhibitor with an IC50 of 2.64 μM. Nevadensin is more selective for hCE1 than hCE2 (IC50 of 132.8 μM). Nevadensin can induce apoptosis and DNA damage in cancer cells. Nevadensin has a variety of pharmacological effects such as anti-inflammatory, anti-tumour, anti-hypertensive, anti-tubercular, antitussive, antioxidant and anti-microbial activities.
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GR148672X
0 ImagesGR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis.
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Isolicoflavonol
0 ImagesIsolicoflavonol potently inhibits hCES2A (Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM.
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Dihydromethysticin
0 ImagesSynonyms: (+)-DihydromethysticinDihydromethysticin is an orally active natural active ingredient. Dihydromethysticin can be extracted from Piper methysticum. Dihydromethysticin inhibits carboxylesterase 1 (Ki = 68.2 μM) and CYP2A5. Dihydromethysticin upregulates NLRC3 and induces Apoptosis. Dihydromethysticin exhibits anticancer activity against colorectal cancer and lung adenoma.
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Carboxylesterase-IN-3
0 ImagesCarboxylesterase-IN-3 (compound 4y) is a potent inhibitor of Carboxylesterase Notum with an IC50 less than or equal to 10 nM. Notum is a negative regulator of Wnt signaling acting through the hydrolysis of a palmitoleoylate ester, which is required for Wnt activity. Carboxylesterase-IN-3 has the potential for the research of cancer disease.
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Ethyl phenylglyoxylate
0 ImagesSynonyms: Ethyl benzoylformate; Phenylglyoxylic acid ethyl esterEthyl phenylglyoxylate (Ethyl benzoylformate), the ethyl ester of phenylglyoxylic acid, is used as a synthetic reagent. Ethyl phenylglyoxylate is also a poor substrate but a potent inhibitor of chicken liver carboxylesterase. Additionally, Ethyl phenylglyoxylate exhibits photoreactivity, where its excited triplet carbonyl can initiate intermolecular hydrogen abstraction, radical coupling and cross-linking reactions.
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Human CES1 Enzyme
0 ImagesCat. No.: HY-E70600Human CES1 Enzyme is a recombinantly expressed CES1 enzyme. Human CES1 Enzyme, an enzyme responsible for the hydrolysis of ester- and amide-containing molecules, is mainly expressed in the liver where it is crucial for the processing of active metabolites and is also involved in trans-esterification reactions.
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CES2A-IN-2
0 ImagesCat. No.: HY-173267Purity: 99.16%CES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible and covalent CES2A inhibitor with an IC50 of 0.04 nM for human CES2A. CES2A-IN-2 covalently binds to CES2A by specifically targeting the catalytic serine residue (Ser-228). CES2A-IN-2 can significantly ameliorate Irinotecan-triggered gut toxicity (ITGT) without diminishing the anti-tumor effects of Irinotecan (HY-16562) in tumor-bearing mice.
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1-Methylisatin
0 Images1-Methylisatin is a potent and selective CE (carboxylesterases) inhibitor, with Kis of 38.2 and 5.38 μM for hiCE and hCE1, respectively. 1-Methylisatin interacts with Hb (human adult hemoglobin) by hydrophobic binding and electrostatic attraction. 1-Methylisatin can be used in the study of regulation of agent metabolism in vivo.
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Tanshinone IIA anhydride
0 ImagesCat. No.: HY-N10686CAS No.: 61077-78-9Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a Ki value of 1.9 nM against hCE1 and a Ki value of 1.4 nM against hiCE. Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase, and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies.
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Alisol G
0 ImagesSynonyms: Alisol-G; 25-Anhydroalisol AAlisol G (25-Anhydroalisol A) is a human carboxylesterase 2 (hCES2) inhibitor with an IC50 of 3.85 μM. Alisol G exhibits cytotoxic activity against human cancer cells, antibacterial activity against Gram-positive strains, and anti-hepatitis B virus activity. Alisol G can be used in research related to lung cancer, breast cancer, prostate cancer, bacterial infections, and HBV infections.
