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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
154 Results for "
catalytically active
" in MedChemExpress (MCE) Product Catalog:
Products (154)
154 Results for "catalytically active" in MCE Product Catalog:
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16 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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2 Cited Publications
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TAK-418 is an orally active, blood-brain barrier-penetrant LSD1 inhibitor with a human IC50 of 2.9 nM. TAK-418 irreversibly inhibits LSD1 by forming a compact flavin-FAD adduct with the catalytic domain FAD, blocking the demethylation of H3K4me1/2 and H3K9me1/2 without disrupting the LSD1-GFI1B interaction. TAK-418 restores normally dysregulated brain gene expression and DNA methylation, increases H3K4me1/2/3 and H3K9me2 at the Ucp2 locus, and induces Ucp2 mRNA expression. TAK-418 rescues defective H3K4 histone modifications, normalizes adult neurogenesis, and improves recognition memory, social behavior, and cognition in rodent models. TAK-418 can be used in research related to neurodevelopmental disorders, Alzheimer's disease, and autism spectrum disorders .
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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-P11307
CAS No.: 1334608-28-4
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Sodium oxalate is an orally active dispersant and coordination agent. Sodium oxalate causes mitochondrial dysfunction. Sodium oxalate has catalytic enhancing activity. Sodium oxalate induces stable chronic kidney disease. Sodium oxalate induces highly malignant and undifferentiated breast tumors .
Cat. No.: HY-153701S
CAS No.: 2417135-66-9
Synonyms: Envudeucitinib; ESK-001
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Envudeucitinibum (Envudeucitinib; ESK-001) is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases .
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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-W002925
CAS No.: 213697-53-1
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DavePhos is a phosphine ligand and electron donor. DavePhos can form cationic rhodium complexes to promote the selective hydrocarboxylation of styrene derivatives with CO2 and H2. As a sacrificial electron donor, DavePhos assists in generating active Rh-H species to initiate the catalytic cycle. DavePhos can be used in Buchwald−Hartwig cross-coupling reactions within palladium-based catalytic systems. DavePhos is applicable to platinum-catalyzed reductive amination of amine-acid .
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Natural Products Metabolic Disease Plants Other Families Extract Endogenous metabolite Disease Research Fields
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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
