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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
49 Results for "
catalytically active site
" in MedChemExpress (MCE) Product Catalog:
Products (49)
49 Results for "catalytically active site" in MCE Product Catalog:
14
14 Cited Publications
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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 .
Cat. No.: HY-134136A
CAS No.: 324518-20-9
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-171036
CAS No.: 252212-58-1
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GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC50 of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD +, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .
Cat. No.: HY-P10422A
Synonyms: ML-peptide, Multi-Leucine (ML)-peptide triacetate
Cat. No.: HY-N10686
CAS No.: 61077-78-9
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Cat. No.: HY-W028350
CAS No.: 40106-12-5
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NSC727447 is a vinyl urea-based allosteric inhibitor of HIV reverse transcriptase-associated RNase H with IC50 values of 2.0 μM and 2.5 μM against HIV-1 and HIV-2 RNase H, respectively, and IC50 values of 100 μM and 10.6 μM against Escherichia coli and human RNase H, respectively. NSC727447 exerts allosteric inhibitory effects mainly by interacting with the region adjacent to α-helix I in the thumb subdomain of the p51 subunit of HIV-1 reverse transcriptase. Cys280, Lys281 and the RNase H primer grip region are involved in its action, and it may inhibit the catalytic activity of RNase H by altering the positioning of nucleic acid substrates or the geometry of the RNase H active site. NSC727447 can be used in studies related to HIV infection, the function of HIV reverse transcriptase RNase H, and allosteric inhibition mechanisms .
Cat. No.: HY-122142A
CAS No.: 127428-47-1
Synonyms: S-2366 (hydrochloride)
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Pyr-Pro-Arg-pNA (S-2366) hydrochloride is a chromogenic peptidyl substrate, and a noncompetitive inhibitor that occupies the active sites of FXIa and FXIa-LC to block factor IX activation. Pyr-Pro-Arg-pNA hydrochloride functions as a hydrolyzable substrate for FXIa’s catalytic domain, human APC, murine APC, and purified plasma kallikrein .
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Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
Cat. No.: HY-D2188
Cat. No.: HY-174423
CAS No.: 1994348-72-9
Synonyms: NC-656
Iptriazopyrid is a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, with a Ki value of 24.3 nM against Arabidopsis thaliana and 33.3 nM against Oryza sativa. Iptriazopyrid binds to the active pocket of HPPD, occupies the catalytic site, inhibits carotenoid biosynthesis, prevents chloroplast formation, and induces albino and chlorotic symptoms in sensitive plants. Used as a herbicide, Iptriazopyrid can control barnyardgrass when applied alone, and its efficacy does not decrease when mixed with labeled residual herbicides. When Iptriazopyrid is mixed with 2,4-D or triclopyr, its barnyardgrass control effect shows an antagonistic effect. Iptriazopyrid is a triazole carboxamide herbicide that exhibits selectivity for Oryza sativa over Echinochloa crus-galli, and has partial tank-mix compatibility with synthetic auxin herbicides registered for rice .
Cat. No.: HY-N15159
CAS No.: 146776-30-9
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Cat. No.: HY-170920
CAS No.: 3056059-99-2
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Herbicide safener-4 is a herbicide safener targeting acetolactate synthase (ALS). Herbicide safener-4 competitively binds to the active site of ALS, blocks the binding of Mesosulfuron-methyl (HY-126987), and simultaneously allows substrates to enter for catalytic reactions. Herbicide safener-4 increases the content/activity of glutathione (GSH), glutathione S-transferase (GST), cytochrome P450 monooxygenase (CYP450) and peroxidase (POD) in plants, and decreases the activity of superoxide dismutase (SOD) .
Cat. No.: HY-10572A
CAS No.: 154801-74-8
Synonyms: (R)-DMP 266; (R)-EFV; (R)-L-743726
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(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
Cat. No.: HY-122142
CAS No.: 72194-57-1
Synonyms: S-2366
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Pyr-Pro-Arg-pNA (S-2366) is a chromogenic peptidyl substrate, and a noncompetitive inhibitor that occupies the active sites of FXIa and FXIa-LC to block factor IX activation. Pyr-Pro-Arg-pNA functions as a hydrolyzable substrate for FXIa’s catalytic domain, human APC, murine APC, and purified plasma kallikrein .
Cat. No.: HY-P10422
CAS No.: 1413058-07-7
Synonyms: ML-peptide, Multi-Leucine (ML)-peptide
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-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-157527
CAS No.: 2978613-03-3
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hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
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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
