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].

References:

[1]. Wang D, et al. Human carboxylesterases: a comprehensive review. Acta Pharm Sin B. 2018 Sep;8(5):699-712. [Content Brief]

Carboxylesterase (CES) Isoform Specific Products:

Carboxylesterase (CES) Isoform Comparison

Carboxylesterase (CES) Related Products (51)
Carboxylesterase (CES) Isoform Comparison

By Effects:	Inhibitors (34) Substrates (2) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-N0235

Bakuchiol	Inhibitor	99.25%
Bakuchiol 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.

HY-N1951

Miltirone	Inhibitor	99.54%
Miltirone 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; K_i = 0.04 μM) and SARS-CoV main protease (Mpro).

HY-114879

DDAO
DDAO 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.

HY-110148

WWL113	Inhibitor	99.72%
WWL113 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).

HY-120602

WWL229		99.49%
WWL229 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.

HY-124446

Dibromsalicil	Inhibitor
Dibromsalicil (Compound 31) is a carboxylesterase (CES) inhibitor with activity of 72.7 nM against hiCE (human intestinal carboxylesterase) and 53.5 nM against rCE (rabbit liver carboxylesterase). Dibromsalicil has almost no activity against hCE1 (human liver carboxylesterase) and cholinesterase.

HY-182632

LP-935001	Inhibitor
LP-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.

HY-W275793

Tripropionin	Substrate
Tripropionin (Glycerol tripropionate) is a triglyceride that can be hydrolyzed by carboxylic esterase from carrots. Tripropionin can serve as the oil phase for constructing high-performance lipid nanoemulsion droplets, enabling efficient encapsulation of Combretastatin A4 (HY-N2146) to achieve its stable storage and controlled release.

HY-N1377

Nevadensin	Inhibitor	99.93%
Nevadensin (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.

HY-110390

GR148672X	Inhibitor	99.58%
GR148672X 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.

HY-N3474

Isolicoflavonol		99.70%
Isolicoflavonol 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.

HY-N0921

Dihydromethysticin	Inhibitor	99.71%
Dihydromethysticin is an orally active natural active ingredient. Dihydromethysticin can be extracted from Piper methysticum. Dihydromethysticin inhibits carboxylesterase 1 (K_i = 68.2 μM) and CYP2A5. Dihydromethysticin upregulates NLRC3 and induces Apoptosis. Dihydromethysticin exhibits anticancer activity against colorectal cancer and lung adenoma.

HY-142689

Carboxylesterase-IN-3	Inhibitor	98.27%
Carboxylesterase-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.

HY-155181

CES2-IN-1	Inhibitor	99.93%
CES2-IN-1 (Compound 24) is a reversible and selective CES2 inhibitor (IC₅₀: 6.72 μM for human CES2). CES2-IN-1 reduces the level of CES2 in living cells. CES2-IN-1 is effective against Irinotecan (HY-16562)-induced delayed diarrhea and DSS-induced ulcerative colitis.

HY-W016618

Ethyl phenylglyoxylate	Inhibitor	99.51%
Ethyl 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.

HY-173267

CES2A-IN-2	Inhibitor	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.

HY-23148

1-Methylisatin		99.81%
1-Methylisatin is a potent and selective CE (carboxylesterases) inhibitor, with K_is 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.

HY-N10686

Tanshinone IIA anhydride	Inhibitor
Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a K_i value of 1.9 nM against hCE1 and a K_i 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.

HY-N0855

Alisol G	Inhibitor	98.13%
Alisol 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.

HY-E70600

Human CES1 Enzyme
Human 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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Carboxylesterase (CES)

Carboxylesterase (CES) Isoform Specific Products:

Carboxylesterase (CES) Isoform Specific Products:

Carboxylesterase (CES) Related Products (51)

Carboxylesterase (CES) Isoform Comparison

Carboxylesterase (CES) Related Products (51):