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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 .
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 .
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 .
Carboxylesterase-IN-1, a novel pesticide, exhibits inhibitory action on carboxylesterase at 50 μg/mL similar to the known inhibitor triphenyl phosphate.
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 .
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively .
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) .
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 .
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 .
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias .
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 .
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 .
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .
Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
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 phosphate diammonium is a fluorescent phosphatase substrate. DDAO phosphate diammonium has tunable excitation wavelength (600-650nm) and long emission wavelength (λem=656nm). DDAO phosphate diammonium can be used to detect the activity of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterase.
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 .
SRE-II, an amide derivative, is an activatable photosensitizer for photodynamic cancer research with decreased fluorescence and photosensitizing capabilities. SRE-II can be further converted into the active photosensitizer SDU Red via carboxylesterase-catalyzed amide bond cleavage. SRE-II induces DNA damage and cell apoptosis in the presence of light. SRE-II can act as a promising theranostic agent for triple-negative breast cancer .
Temocapril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases .
Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases .
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 phosphate diammonium is a fluorescent phosphatase substrate. DDAO phosphate diammonium has tunable excitation wavelength (600-650nm) and long emission wavelength (λem=656nm). DDAO phosphate diammonium can be used to detect the activity of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterase.
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively .
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 .
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .
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 .
Carboxylesterase 1 Protein, Human (HEK293, His) is an approximately 60.0 kDa human carboxylesterase 1 protein with a His-flag. Human Carboxylesterase 1 is the key liver microsomal enzyme that takes part in detoxification and metabolism.
CES2, a hydrolase, demonstrates notable activity with palmitoylcarnitine and other substrates like p-nitrophenylacetate and alpha-naphthylacetate. Its versatile enzymatic capabilities extend to the hydrolysis of retinyl esters. CES2/carboxylesterase 2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived CES2/carboxylesterase 2 protein, expressed by HEK293 , with C-His labeled tag. The total length of CES2/carboxylesterase 2 Protein, Mouse (HEK293, His) is 557 a.a., with molecular weight of 52-60 KDa.
The CES2 protein plays a crucial role in detoxifying xenobiotics and activating ester and amide prodrugs. It has high catalytic efficiency, especially in the hydrolysis of substances such as cocaine, 4-methylumbelliferyl acetate, heroin and 6-monoacetylmorphine. CES2/carboxylesterase 2 Protein, Human (HEK293,C-His) is the recombinant human-derived CES2/carboxylesterase 2 protein, expressed by HEK293 , with C-His labeled tag. The total length of CES2/carboxylesterase 2 Protein, Human (HEK293,C-His) is 533 a.a., with molecular weight of ~60.4 KDa.
CES2 Protein plays a crucial role in detoxifying xenobiotics and activating ester and amide prodrugs. It exhibits high catalytic efficiency, particularly in the hydrolysis of substances like cocaine, 4-methylumbelliferyl acetate, heroin, and 6-monoacetylmorphine. Additionally, CES2 participates in the hydrolysis of aspirin, substrates with large alcohol groups and small acyl groups, as well as endogenous lipids such as triacylglycerol. The protein is involved in the conversion of monoacylglycerides to free fatty acids and glycerol and contributes to the hydrolysis of 2-arachidonoylglycerol and prostaglandins. CES2/carboxylesterase 2 Protein, Human (HEK293,C-His,Solution) is the recombinant human-derived CES2/carboxylesterase 2 protein, expressed by HEK293 , with C-10*His labeled tag. The total length of CES2/carboxylesterase 2 Protein, Human (HEK293,C-His,Solution) is 533 a.a., with molecular weight of ~50-70 kDa.
Carboxylesterase 5 Protein, Mouse (HEK293, His) is a mouse Carboxylesterase 5 protein with a His-flag. Carboxylesterase 5 is encoded byCarboxylesterase 5 (CES5) and can catalyses hydrolytic and transesterification reactions.
CES3/CES1D Protein, a major lipase in white adipose tissue, plays a crucial role in xenobiotic and natural substrate metabolism. It hydrolyzes triacylglycerols and monoacylglycerols, showing a preference for the latter, with susceptibility increasing as the acyl chain length decreases. Additionally, CES3/CES1D catalyzes the synthesis of fatty acid ethyl esters and hydrolyzes retinyl esters. CES3/CES1D Protein, Mouse (HEK293, His) is the recombinant mouse-derived CES3/CES1D protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CES3/CES1D Protein, Mouse (HEK293, His) is 543 a.a., with molecular weight of 58-70 kDa.
The carboxylesterase 1C protein is essential for xenobiotic detoxification and ester/amide prodrug activation, as well as participating in extracellular metabolism. Its multifunctional effects include processing of pulmonary surfactant. Carboxylesterase 1C Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived Carboxylesterase 1C protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of Carboxylesterase 1C Protein, Mouse (P.pastoris, His) is 532 a.a., with molecular weight of ~60.6 kDa.
Notum Protein serves as a crucial negative regulator of the Wnt signaling pathway, playing a specific role in mediating the depalmitoleoylation of WNT proteins. The process of serine palmitoleoylation of WNT proteins is essential for their efficient binding to frizzled receptors, and Notum's carboxylesterase activity is instrumental in modulating this aspect of the Wnt signaling cascade. Notum Protein, Human (C330S, CHO, His) is the recombinant human-derived Notum protein, expressed by CHO , with C-His labeled tag. The total length of Notum Protein, Human (C330S, CHO, His) is 371 a.a., with molecular weight of 36-45 kDa.
