2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Carboxylesterase (CES)

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:

Carboxylesterase (CES) Isoform Comparison
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.
    Bakuchiol
  • HY-114879
    DDAO
    		98.43%
    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.
    DDAO
  • HY-N0921
    Dihydromethysticin
    		Inhibitor 99.94%
    Dihydromethysticin 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.
    Dihydromethysticin
  • HY-N1951
    Miltirone
    		Inhibitor 99.74%
    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; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
    Miltirone
  • HY-120602
    WWL229
    		98.55%
    WWL229 is a selective inhibitor of carboxylesterase 3 (Ces3) with an IC50 of 1.94 µM. WWL229 promotes lipid storage in cultured adipocytes and prevents basal lipolysis.
    WWL229
  • HY-173267
    CES2A-IN-2
    		Inhibitor
    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.
    CES2A-IN-2
  • HY-176465
    CES2A-IN-3
    		Inhibitor
    CES2A-IN-3 (Compound 9d) is a potent serine-targeting covalent human carboxylesterase 2A (hCES2A) inhibitor with an IC50 value of 0.12 nM. CES2A-IN-3 is promising for research of diarrhea and ulcerative colitis.
    CES2A-IN-3
  • HY-W701476
    Ethyl phenylglyoxylate-d5
    Ethyl phenylglyoxylate-d5 (Ethyl benzoylformate-d5; Phenylglyoxylic acid ethyl ester-d5) is the deuterium labeled Ethyl phenylglyoxylate (HY-W016618). 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.
    Ethyl phenylglyoxylate-d<sub>5</sub>
  • 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).
    WWL113
  • 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.
    Isolicoflavonol
  • HY-144809
    Pancreatic lipase/Carboxylesterase 1-IN-1
    		99.92%
    Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A) with IC50 values of 2.13 µM and 0.055  µM against PL and hCES1A.
    Pancreatic lipase/Carboxylesterase 1-IN-1
  • 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.
    Nevadensin
  • 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.
    Carboxylesterase-IN-3
  • HY-155181
    CES2-IN-1
    		Inhibitor 98.18%
    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.
    CES2-IN-1
  • HY-23148
    1-Methylisatin
    		99.81%
    1-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.
    1-Methylisatin
  • HY-N10686
    Tanshinone IIA anhydride
    		Inhibitor
    Tanshinone IIA anhydride is a potent and irreversible human carboxylesterase (CE) inhibitor with Ki values of 1.9 nM and 1.4 nM for human CE1 and the human intestinal CE (hiCE), respectively.
    Tanshinone IIA anhydride
  • HY-N3921
    Gancaonin I
    Gancaonin I, an Isoflavone, exhibits moderate inhibition on human carboxylesterase 2 (hCES2A) with IC50 of 1.72 μM. Gancaonin I inhibits hCES2A-mediated fluorescein diacetate (FD) hydrolysis.
    Gancaonin I
  • HY-W016618
    Ethyl phenylglyoxylate
    		Inhibitor 98.31%
    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.
    Ethyl phenylglyoxylate
  • HY-118041
    PMPMEase-IN-1
    		Inhibitor
    PMPMEase-IN-1 is an allylated methylated protein methylesterase inhibitor with the property of inhibiting PMPMEase activity. PMPMEase-IN-1 may provide a useful strategy for cancer inhibition by enhancing its affinity for polyisoprenyl derivatives. PMPMEase-IN-1 showed the potential to have an effective concentration (EC50) value in causing degeneration of human neuroblastoma SH-SY5Y cells. Specific inhibition of PMPMEase-IN-1 may help regulate the metabolism of polyisoprenyl proteins and thus maintain normal cell survival. Further development and application of PMPMEase-IN-1 may open up new avenues for inhibiting degenerative diseases and cancer.
    PMPMEase-IN-1
  • HY-147331
    Oseltamivir acid methyl ester
    		Inhibitor
    Oseltamivir acid methyl ester is a precursor form of the neuraminidase inhibitor and antiviral oseltamivir acid. Oseltamivir acid methyl ester is converted to oseltamivir acid by carboxylesterase 1 (CES1).
    Oseltamivir acid methyl ester
Carboxylesterase (CES) Isoform Comparison

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