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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
18 Results for "
catalytic active site residues
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "catalytic active site residues" in MCE Product Catalog:
Cat. No.: HY-134136A
CAS No.: 324518-20-9
Cat. No.: HY-157521
CAS No.: 3055162-52-9
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Research Areas:
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-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 .
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-110147A
CAS No.: 2320930-10-5
SSM-3 tetraTFA is a potent furin inhibitor with an EC50 of 54 nM. SSM-3 tetraTFA 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 can be used in the research of anthrax and avian influenza .
Cat. No.: HY-187383
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Carbonic anhydrase-IN-40 is a human carbonic anhydrase I/II inhibitor, with an IC50 of 16.900 nM against hCA I and an IC50 of 4.682 nM against hCA II. Carbonic anhydrase-IN-40 binds to the active site of the enzyme, coordinates with the catalytic zinc ion, forms π-π stacking interactions with active site residues, and makes hydrophobic contacts with the hydrophobic pocket. Carbonic anhydrase-IN-40 can serve as a lead compound for studies related to carbonic anhydrase inhibitors .
Cat. No.: HY-P5427
CAS No.: 209004-76-2
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Cat. No.: HY-110147
CAS No.: 922732-52-3
SSM-3 is a potent furin inhibitor with an EC50 of 54 nM. SSM-3 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 can be used in the research of anthrax and avian influenza .
Cat. No.: HY-P0112
CAS No.: 1027141-02-1
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Z-VAE (OMe)-FMK is a selective inhibitor of UCHL1, with better selectivity over UCHL3 and UCHL5. Z-VAE (OMe)-FMK binds to the active site cleft, covalently modifies the active site cysteine C90 to form a thioether bond, binds to inactive UCHL1 with a misaligned catalytic triad, and acts via a two-step addition-folding/migration/displacement mechanism. Z-VAE (OMe)-FMK stabilizes interactions through hydrogen bonding with oxyanion hole residues and van der Waals interactions with surrounding residues. Z-VAE (OMe)-FMK can be used in research related to colorectal cancer, lung cancer, pancreatic cancer, and Alzheimer's disease .
Cat. No.: HY-187174
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CA IX-IN-6 is a selective human carbonic anhydrase IX (hCA IX) inhibitor, with Ki values of 8.9, 50.7, 551, and 64.4 nM against hCA IX, hCA XII, hCA I, and hCA II, respectively. CA IX-IN-6 binds to the active site via a classic sulfamide mode, coordinates with the catalytic Zn 2+ ion, forms a hydrogen bond with Thr200, and interacts with key active site residues. CA IX-IN-6 can be used in studies related to tumor-associated carbonic anhydrase inhibition .
Cat. No.: HY-115373
CAS No.: 112105-54-1
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RO314724 is a selective MMP-1 inhibitor. RO314724 chelates to the catalytic zinc ion within the active site of MMP-1 and forms a stable complex with MMP-1. RO314724 can be used for the research of osteoarthritis .
Cat. No.: HY-189207
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NUDT1-IN-1 is an inhibitor of NUDT1 (MTH1) with a pIC50 value of 9.785. NUDT1-IN-1 can be applied in cancer research .
Cat. No.: HY-186236
CAS No.: 892706-90-0
N42FTA is a non-covalent, non-suicidal inhibitor of FabA from Pseudomonas aeruginosa and Escherichia coli, with IC50 values of 3.27 μM and 2.31 μM, respectively. As a natural substrate mimetic, N42FTA blocks the cross-linking between acyl carrier protein and FabA in Escherichia coli. N42FTA shows no significant antibacterial activity due to poor permeability. N42FTA can be used in studies related to Pseudomonas aeruginosa and Escherichia coli infections .
Cat. No.: HY-189205
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DKFZ-938 is a kallikrein-related peptidase 6 (KLK6) inhibitor, with an IC50 of 0.09 μM against human KLK6. DKFZ-938 binds to the catalytic serine residue in the active-site pocket of KLK6 and mimics the natural KLK6 substrate to inhibit the enzymatic activity of KLK6. DKFZ-938 can be conjugated to the non-canonical amino acid propargyllysine via copper-catalyzed azide-alkyne cycloaddition click chemistry. DKFZ-938 is used in research related to colorectal cancer and pancreatic cancer .
Cat. No.: HY-117641
CAS No.: 121584-61-0
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CP 81282 is a tripeptide aspartic protease inhibitor, with an IC50 of 1 nM against human renin and an IC50 of 11 nM against endopeptidase. CP 81282 is applicable to the research of hypertension .
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 .
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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
