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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
1215 Results for "
Enzyme activity
" in MedChemExpress (MCE) Product Catalog:
Products (1215)
1215 Results for "Enzyme activity" in MCE Product Catalog:
Cat. No.: HY-165426
CAS No.: 3031522-14-9
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HB-230 is a Transglutaminase-2 (TG2) (human IC50 = 4.9 μM) inhibitor and a selective fluorescent imaging probe for active TG2 localization. HB-230 modifies TG2 Cys277 to sustain the enzyme open conformation. HB-230 forms a ternary complex with TG2 and α2-macroglobulin, undergoes receptor-mediated endocytosis, and trafficks directly to lysosomes without early/late endosome fusion. HB-230 exhibits TG2 activity-dependent and α2-macroglobulin-dependent uptake. HB-230 can be used for the research of celiac disease, (Ex/Em = 649/665 nm) .
Cat. No.: HY-177543
CAS No.: 65490-84-8
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5-(4-Methoxyphenol)-4-methyl-3H-1,2-dithiole-3-thione is a Phase 2 enzyme inducer. 5-(4-Methoxyphenol)-4-methyl-3H-1,2-dithiole-3-thione induces the activity of NAD (P) H:quinone oxidoreductase (QR; NQO1) in hepatoma cells. 5-(4-Methoxyphenol)-4-methyl-3H-1,2-dithiole-3-thione enhances growth hormone production in plasmid-transfected hepatoma cells .
Cat. No.: HY-184980
CAS No.: 2180967-88-6
Urease-IN-23 is a cryptococcal urease inhibitor with antifungal activity. AF55 exhibits mixed-type inhibition against cryptococcal urease, binds to both the nickel ion site at the enzyme's catalytic center and the allosteric site, impairs urease catalytic efficiency, simultaneously disrupts fungal virulence structures and damages cell membrane integrity. The IC50 and Ki values of Urease-IN-23 against cryptococcal urease are 54.92 nM and 149.1 nM, respectively. Urease-IN-23 significantly reduces the capsule thickness of Cryptococcus neoformans and Cryptococcus gattii, increases fungal cell membrane permeability, and completely blocks melanin synthesis. Urease-IN-23 shows no toxicity in the Galleria mellonella larval model. Urease-IN-23 can be used in studies related to fungal infections .
Synonyms: Glyoxaline (Standard); 1,3-Diaza-2,4-cyclopentadiene (Standard)
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Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
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Sudan IV (Standard) (Solvent Red 24 (Standard)) is the analytical standard of Sudan IV (HY-D0932). This product is intended for research and analytical applications. Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.
Cat. No.: HY-N19401
CAS No.: 36001-47-5
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Rutaceae Extract Microorganisms Gibberellins Other Diseases Plants Phytohormone Disease Research Fields Citrus reticulata Blanco Agricultural Research
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Cardiovascular Disease Alkaloids Phenols Polyphenols Nymphaeaceae Extract Nelumbo nucifera Gaertn. Plants Disease Research Fields Isoquinoline Alkaloids
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Cat. No.: HY-P10302A
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Cat. No.: HY-P10819
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Phosphofructokinase 1 (PFK1) is a glycolytic enzyme and also an allosteric activation target of fructose-2,6-bisphosphate. PFK1 supports cardiac glycolysis to maintain normal cardiac function and mediates adaptive responses to pressure overload. Upregulated expression and activity of PFK1 are associated with the alleviation of pathological changes induced by pressure overload, including diastolic dysfunction, interstitial fibrosis and myocardial hypertrophy. Inhibition of PFK1 redirects glucose carbon flux to the pentose phosphate pathway. PFK1 promotes proliferation, migration and glycolysis of colorectal cancer cells, reduces apoptosis and decreases their radiosensitivity, and shows higher expression levels in radioresistant tumors. PFK1 can be used in research related to diastolic dysfunction heart failure and colorectal cancer .
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Phosphofructokinase,Bacillus stearothermophilus is a glycolytic enzyme and also an allosteric activation target of fructose-2,6-bisphosphate. PFK1 supports cardiac glycolysis to maintain normal cardiac function and mediates adaptive responses to pressure overload. Upregulated expression and activity of PFK1 are associated with the alleviation of pathological changes induced by pressure overload, including diastolic dysfunction, interstitial fibrosis and myocardial hypertrophy. Inhibition of PFK1 redirects glucose carbon flux to the pentose phosphate pathway. PFK1 promotes proliferation, migration and glycolysis of colorectal cancer cells, reduces apoptosis and decreases their radiosensitivity, and shows higher expression levels in radioresistant tumors. PFK1 can be used in research related to diastolic dysfunction heart failure and colorectal cancer .
Cat. No.: HY-P990951
CAS No.: 2845128-05-2
Synonyms: REGN-5381
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Cat. No.: HY-W490804
CAS No.: 2971-36-0
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HPTE is the active in vivo metabolite of Methoxychlor (HY-B1873), and acts as an inhibitor of 3β‑HSD and 17β‑HSD3. HPTE binds to the substrate-binding pocket of 3β‑HSD in a non-competitive manner, but competitively occupies the coenzyme NAD +-binding site, thereby inhibiting the conversion of pregnenolone to progesterone. HPTE binds to the androstenedione-binding pocket (the substrate pocket) of 17β‑HSD3 in a non-competitive manner, and competitively occupies the coenzyme NADPH-binding site, thus blocking the conversion of androstenedione to testosterone. HPTE interferes with androgen biosynthesis in Leydig cells by inhibiting the activities of these two key steroidogenic enzymes. HPTE can be used in studies related to androgen biosynthesis .
Cat. No.: HY-W663179
CAS No.: 681492-17-1
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DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
Cat. No.: HY-W699983
CAS No.: 74362-46-2
Synonyms: Glyoxaline-15N2; 1,3-Diaza-2,4-cyclopentadiene-15N2
Cat. No.: HY-L230
331 compounds
Kinases are enzymes that catalyze the addition of phosphate groups to substrate molecules, a process known as phosphorylation. Protein phosphorylation serves as a critical regulatory mechanism for numerous cellular processes, including cell division, metabolism, and signal transduction. The human genome encodes over 500 kinases, which collectively regulate approximately 50% of cellular functions. Due to their pivotal roles, kinases represent one of the most important target classes in drug development.
Kinase inhibitors can selectively block the activity of disease-associated kinases, making them valuable therapeutics for conditions such as cancer and inflammatory diseases. FDA-approved kinase inhibitors have undergone extensive preclinical and clinical studies, demonstrating high bioactivity, favorable safety profiles, and good bioavailability, rendering them suitable for investigating new therapeutic indications.
Cat. No.: HY-121501
CAS No.: 121024-51-9
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Tyrostatin is a peptide inhibitor isolated from Kitasatospora sp. 55. It has a Ki value of 6 nM against serine carboxyl protease (PSCP) from Pseudomonas sp. 101, a Ki value of 2.1 nM against carboxyl protease (XSCP) from Xanthomonas sp. T-22, and a Ki value of 2.6 nM against carboxyl protease (PCP) from Pseudomonas sp. 101. Tyrostatin forms a reversible covalent hemiacetal bond with Ser287 at the active site of PSCP, where Tyr at the P1 position and Leu at the P2 position occupy the S1-S4 subsites of the enzyme. Tyrostatin inhibits the activity of XSCP, specifically blocks the autocatalytic maturation process of PCP precursor under acidic conditions, and also inhibits the protease activity of mature and recombinant PCP in a dose-dependent manner. Tyrostatin does not inhibit KSCP or alcohol-resistant protease J-4, and can serve as a tool for identifying the catalytic residues of PCP .
Cat. No.: HY-189662
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Y-U0-S is a potent inhibitor of the coronavirus main protease (M pro) and host cathepsins. The IC50 values of Y-U0-S against SARS-CoV-2 M pro, SARS-CoV Mpro, Cathepsin B, and Cathepsin L are 0.81, 1.14, 0.86, and 21.13 μM, respectively. Y-U0-S exhibits broad-spectrum anti-coronavirus activity, with an EC50 of 0.22 μM against wild-type SARS-CoV-2. Y-U0-S forms an irreversible covalent bond with the catalytic site C145 of M pro through its aldehyde warhead, and by optimizing multi-site occupancy of the scaffold to engage conserved residues, it effectively blocks enzyme activity and inhibits viral replication. Y-U0-S can be used for research on COVID-19 .
Cat. No.: HY-B1451R
CAS No.: 89396-94-1
Synonyms: TA-6366 (Standard)
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Imidapril (hydrochloride) (Standard) is the analytical standard of Imidapril (hydrochloride). This product is intended for research and analytical applications. Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
