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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
26 Results for "
serine active site
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "serine active site" in MCE Product Catalog:
16
16 Publications Verification
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PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .
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1 Cited Publications
Cat. No.: HY-P701745
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: PIM1; Proto-Oncogene serine/Threonine-Protein Kinase Pim-1; Prev. PIM; Pim-1 Oncogene; serine/Threonine-Protein Kinase Pim-1; Oncogene PIM1; Pim-1 Proto-Oncogene, serine/Threonine Kinase; Pim-1 Oncogene (Proviral Integration site 1)
Species:
Human
Source:
E. coli
NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
Category:
Microorganisms Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields
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DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD +/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers .
Cat. No.: HY-153552
CAS No.: 2758337-19-6
NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
Cat. No.: HY-N10686
CAS No.: 61077-78-9
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Cat. No.: HY-126031
CAS No.: 2055172-60-4
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(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
Cat. No.: HY-P5455
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Cat. No.: HY-B1863
CAS No.: 26087-47-8
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Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos can phosphorylate the -OH group on the serine residue in the active (esteratic) site of ChEs and so inhibit both AChE and BChE activity .
Cat. No.: HY-162094
CAS No.: 3027135-80-1
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CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis .
Cat. No.: HY-176001
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DPP8/9-IN-1 (Compound 16) is a selective covalent inhibitor of dipeptidyl peptidases 8 and 9 (DPP8/9) with IC50 values of 14 and 298 nM, respectively. DPP8/9-IN-1 binds irreversibly to the active site serine (S730 in DPP9) via a phosphonate warhead and blocks substrate binding to inhibit DPP8/9-mediated protein processing. DPP8/9-IN-1 is promising for research of cancers and inflammatory diseases .
Cat. No.: HY-171781
CAS No.: 693235-40-4
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FL-166 is a SARS coronavirus main protease (Mpro) inhibitor (Ki: 40 nM). FL-166 exerts its inhibitory effect by targeting a cluster of serine residues near the active site of the protease. FL-166 can be used in the study of SARS-CoV .
Cat. No.: HY-B1863R
CAS No.: 26087-47-8
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Iprobenfos (Standard) is the analytical standard of Iprobenfos (HY-B1863). This product is intended for research and analytical applications. Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos can phosphorylate the -OH group on the serine residue in the active (esteratic) site of ChEs and so inhibit both AChE and BChE activity .
Cat. No.: HY-W728451
CAS No.: 904672-77-1
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URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare 11C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH .
Cat. No.: HY-129284
CAS No.: 209125-28-0
APHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition .
Cat. No.: HY-16183A
CAS No.: 120087-68-5
Synonyms: Echothiophate chloride
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Echothiophate (Echothiophate) chloride is a highly effective, long-lasting cholinesterase inhibitor employed as a miotic for managing glaucoma. Echothiopate chloride forms a covalent bond with the serine residue at the active site of cholinesterase through its phosphate group, rendering the enzyme permanently inactive and necessitating the synthesis of new enzymes by the cell. Given its irreversible binding to cholinesterase and the extremely slow rate of hydrolysis, the effects of echothiophate can persist for a week or longer. Echothiopate chloride is utilized as an ocular antihypertensive agent in the treatment of chronic glaucoma and, in certain cases, accommodative esotropia.
Cat. No.: HY-P992451
Synonyms: KY1066
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Cat. No.: HY-185905
CAS No.: 1811556-64-5
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TTAMRA-FP is an activity-based probe for serine hydrolases (Serine Hydrolase) that irreversibly and covalently labels the active-site serine of catalytically active serine hydrolases. TTAMRA-FP can be used for activity-based protein profiling of serine hydrolases and related studies on the activity of osteoarthritis-associated proteases .
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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
