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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
120 Results for "
catalytic sites
" in MedChemExpress (MCE) Product Catalog:
Products (120)
120 Results for "catalytic sites" in MCE Product Catalog:
38
38 Publications Verification
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
38
38 Publications Verification
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
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 .
6
Dihydroergotamine mesylate is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine mesylate inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine mesylate binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine mesylate can be used in studies related to migraine and trypanosome infections .
1
1 Cited Publications
KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer .
Cat. No.: HY-161762
CAS No.: 3038542-51-4
Synonyms: RA-2034
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RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with an IC50 of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner .
Cat. No.: HY-N6675
CAS No.: 94238-00-3
Category:
Natural Products Neurological Disease Lridaceae Plants Crocus sativus L. Disease Research Fields Cancer
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FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase .
Cat. No.: HY-P3823
CAS No.: 145224-96-0
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Cat. No.: HY-P5979
CAS No.: 1071466-49-3
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5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively .
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 .
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Triosephosphate isomerase (TPI) is a biocatalyst that interconverts dihydroxyacetone phosphate and D-glyceraldehyde-3-phosphate. Triosephosphate isomerase utilises Glu167 as catalytic base, mediates proton shuttling, and stabilises a cis-enediolate intermediate via loop-6 and loop-7 closure to shield its catalytic site. Triosephosphate isomerase can be used for the research of triosephosphate isomerase deficiency .
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DMNB-caged-Serine is a photocaged amino acid. DMNB-caged-Serine can be used as a catalytic residue, hydrogen bonding partner or site of post-translational modification. DMNB-caged-Serine can be used for the control of protein phosphorylation .
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-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 .
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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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 .
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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
