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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
79 Results for "
active site residues
" in MedChemExpress (MCE) Product Catalog:
Products (79)
79 Results for "active site residues" in MCE Product Catalog:
5
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Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect .
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I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes.?I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST .
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2 Cited Publications
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MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .
1
Cat. No.: HY-134136A
CAS No.: 324518-20-9
Synonyms: NCGC-00183434
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ML132 (NCGC-00183434) is a selective caspase 1 inhibitor with an IC50 value of 0.023 nM. ML132 has good stability and can be used as a caspase 1 molecular probe. ML132 is applicable to research in the fields of anticancer and anti-inflammatory studies .
Cat. No.: HY-157521
CAS No.: 3055162-52-9
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AANAT-IN-1 is an arylalkylamine N-acetyltransferase (AANAT) inhibitor with a sheep AANAT IC50 of 9.9 μM. AANAT-IN-1 binds to the active site of sheep AANAT, interacting with amino acid residues via hydrogen bonds, hydrophobic interactions, ionic interactions, and water bridges, inhibiting the enzyme's catalytic activity. AANAT-IN-1 can be used for the researches of circadian rhythm-associated neuropsychiatric conditions, seasonal affective disorder, and other diseases associated with abnormally elevated melatonin levels .
Cat. No.: HY-N1341
CAS No.: 54835-70-0
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Roseoside is an inhibitor of DNA gyrase and HAV 3C protease, and also inhibits HCV NS5A/B replicase in human systems with an IC50 of 20 μM. Roseoside binds to the active site of enzymes and stabilizes the interaction by forming hydrogen bonds with key amino acid residues. Roseoside inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, and Candida albicans, and interferes with HCV RNA replication in vitro by inhibiting HCV NS5A/B replicase (IC50=20 μM). Roseoside shows no cytotoxicity and serves as a research tool for studies related to bacterial infections, candidiasis, HAV and HCV .
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Infection Cardiovascular Disease Inflammation/Immunology Cancer
Thioredoxin reductase (TrxR) is a selenoprotein that plays a central role in cellular redox homeostasis by utilizing highly reactive selenocysteine (Sec) residues exposed to solvents at its active site. Thioredoxin reductase can be used for the study of diverse diseases, from rheumatoid arthritis and ischemia to cancer and parasitic infections .
Cat. No.: HY-110172
CAS No.: 1461648-55-4
PDI-IN-1 is a cell-permeable PDI covalent inhibitor with an IC50 of 1.7 μM against bovine PDI. PDI-IN-1 specifically modifies the Cys397 residue at the active site of human PDI, selectively labels endogenous PDI in living mammalian cancer cells, and effectively inhibits PDI-mediated insulin aggregation in vitro. PDI-IN-1 exhibits significant anti-tumor activity and inhibits the growth of various cancer cell lines .
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8RK64 is a UCHL1 inhibitor that covalently binds the active-site cysteine residue to form an isothiourea adduct, with selectivity over UCHL3, UCHL5, and other cysteine DUBs. 8RK64 inhibits human UCHL1 with an IC50 of 0.32 μM. 8RK64 is an azide-containing precursor usable as a two-step activity-based probe via click chemistry. 8RK64 can be used for the research of Parkinson's disease .
Cat. No.: HY-N10423
CAS No.: 18423-69-3
Synonyms: (-)-Cubebin
Cat. No.: HY-W000854
CAS No.: 10365-98-7
Synonyms: 3-Methoxyphenylboronic acid
Cat. No.: HY-110147B
Purity: ≥99.0%
SSM-3 tetraTFA hydrate is a potent furin inhibitor with an EC50 of 54 nM. SSM-3 tetraTFA hydrate uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 tetraTFA hydrate can be used in the research of anthrax and avian influenza .
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Papaveroline is a Fyn tyrosine kinase inhibitor, Na +,K +-ATPase inhibitor with an IC50 of 0.20 mM, Mg 2+-ATPase inhibitor, K +-activated pNPPase inhibitor with an IC50 of 1.51 mM, and apoptosis inducer . Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues . Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels . Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease . Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease .
Cat. No.: HY-175249
CAS No.: 3082627-31-1
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TKL-IN-2 is a herbicide and SvTKL inhibitor with an IC50 of 0.11 mg/L. TKL-IN-2 binds to the SvTKL active site, interacts with key pocket residues, and inhibits enzyme activity. TKL-IN-2 can be used for the research of weed control in maize, wheat, soybean, and cotton fields .
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-124308
CAS No.: 1221964-50-6
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
Cat. No.: HY-175031
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GRL-07524 (Compound 4e) is a potent inhibitor of HIV-1 protease (Ki = 0.22 nM). GRL-07524 contains oxaspirocyclic carbamates as the P2 ligands. GRL-07524 exhibits good antiviral activity with an EC50 = 210 nM. GRL-07524 binds to the HIV-1 PR active site in one of the four symmetry independent molecules along with key catalytic residues .
Cat. No.: HY-174438
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PSEC13 is an activator of HSF-1/DAF-16 axis. PSEC13 can upregulate heat shock proteins. PSEC13 can form hydrogen bonds with key residues in the HSP-16.2 active site. PSEC13 can be used to enhance proteostasis and extend lifespan through the modulation of HSP-16.2. PSEC13 could promote the nuclear translocation of daf-16, upgrading the proportion of intermediate. PSEC13 can be studied in research for aging and age-related diseases .
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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
