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

Carboxylesterase (CES) Inhibitor

Carboxylesterase (CES) Isoform Comparison

Carboxylesterase (CES) Inhibitors (34):

Cat. No. Product Name Effect Purity
  • 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; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
  • 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-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-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-N0921
    Dihydromethysticin
    		Inhibitor 99.71%
    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.
  • 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-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 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.
  • 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-142688
    Carboxylesterase-IN-2
    		Inhibitor 99.91%
    Carboxylesterase-IN-2 (compound 4u) 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-2 has the potential for the research of cancer disease.
  • 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.
  • 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).
  • HY-147915
    Benz-AP
    		Inhibitor
    Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids.
  • 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.
  • HY-169068
    Antifeedant agent 1
    		Inhibitor
    Antifeedant agent 1 is a carboxylesterase inhibitor that exerts insecticidal activity by inhibiting insect feeding, with an EC50 value of 0.038 mg/mL. Antifeedant agent 1 can be used in research related to pest control.