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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
101 Results for "
Catalytic domain
" in MedChemExpress (MCE) Product Catalog:
Products (101)
101 Results for "Catalytic domain" in MCE Product Catalog:
8
8 Cited Publications
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GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP47 and Ub-MDM2, respectively .
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NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
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3 Cited Publications
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USP5-IN-1 (compound 64) is a selective competitive inhibitor of USP5 zinc finger ubiquitin binding domain (ZnF-UBD) (KD=2.8 μM). USP5-IN-1 competitively blocks the binding of ubiquitin to ZnF-UBD, inhibits the catalytic activity of USP5, and thus hinders the hydrolysis of ubiquitin chains. USP5-IN-1 can inhibit USP5 cleavage of Lys48-linked diubiquitin substrates in vitro and is a potential USP5 chemical probe and potential inhibitor of USP5-related cancers.
2
2 Cited Publications
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COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors .
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2 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 .
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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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BAY-524 is a potent Bub1 kinase inhibitor. BAY-524 inhibits the recombinant catalytic domain of human Bub1 with an IC50 of 450 nM. BAY-524 can be used for the research of anti-cancer in combination with other agents .
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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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2 Cited Publications
Synonyms: 6-Methyladenosine (Standard); N-Methyladenosine (Standard)
1
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 .
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1 Cited Publications
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XL 188 is a potent and selective USP7 inhibitor with IC50 values of 90 nM and 193 nM for USP7 full-length and catalytic domain enzyme, respectively. XL 188 can be used in research of cancer .
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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 .
Cat. No.: HY-P99415
CAS No.: 2098724-83-3
Synonyms: MAA868
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L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment .
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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TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively .
Cat. No.: HY-130245
Purity: 98.33%
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PCSK9 degrader 1 is a HyT-like PCSK9 degrader with a Ki of 107 nM. PCSK9 degrader 1 binds to the allosteric pocket between the catalytic domain and C-terminal domain of PCSK9. While maintaining key interactions with this protein, it extends the proteasome-recruiting moiety, thereby driving degradation via the proteasomal pathway. PCSK9 degrader 1 induces the degradation of both the precursor and mature forms of PCSK9, with DC50 values of 4.8 μM and 3.4 μM respectively, and does not significantly affect cell viability or the expression of housekeeping proteins. PCSK9 degrader 1 can be used in the research of coronary heart disease .
Cat. No.: HY-163144
CAS No.: 3044084-97-8
DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia .
Cat. No.: HY-P10939A
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Cat. No.: HY-N10159
CAS No.: 60941-76-6
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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
