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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
127 Results for "
catalytically active
" in MedChemExpress (MCE) Product Catalog:
Products (127)
127 Results for "catalytically active" in MCE Product Catalog:
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14 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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RG3039 (PF-06687859) is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 extends survival and improves function in spinal muscular atrophy mice. RG3039 is applicable to research related to spinal muscular atrophy .
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3 Cited Publications
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
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Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor. The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .
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1 Cited Publications
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Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors .
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1 Cited Publications
Cat. No.: HY-G0017
CAS No.: 404844-02-6
Synonyms: Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588
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N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
Cat. No.: HY-E70069
CAS No.: 37278-88-9
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Endo-β-N-acetylglucosaminidase (Endo S2) is a key enzyme involved in the processing of free oligosaccharides in the cytosol. Endo-β-N-acetylglucosaminidase catalyzes hydrolysis of N-linked oligosaccharides .
Cat. No.: HY-P11307
CAS No.: 1334608-28-4
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Cat. No.: HY-134136A
CAS No.: 324518-20-9
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Microbial neutral proteinase is a zinc-containing metalloproteinase mainly produced by Bacillus and fungi. Its catalytic activity is highly dependent on divalent cations, and it remains active within the pH range of 5-8. Microbial neutral proteinase can specifically cleave peptide bonds within polypeptide chains, thereby degrading macromolecular proteins into small peptides or amino acids. It can be applied in various industrial fields including food processing, brewing, detergents, and light industry .
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-P5489
CAS No.: 849069-99-4
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Cat. No.: HY-P10422A
Synonyms: ML-peptide, Multi-Leucine (ML)-peptide triacetate
Cat. No.: HY-24312
CAS No.: 153130-59-7
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 .
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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
