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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
16 Results for "
DCN1 inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "DCN1 inhibitor" in MCE Product Catalog:
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4 Cited Publications
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NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .
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2 Cited Publications
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DI-1859 is a DCN1 and cullin 3 inhibitor with a Ki of <1 nM against human DCN1. DI-1859 forms a covalent bond with Cys115 of DCN1, cleaves its dimethylamino group, disrupts the DCN1-UBC12 interaction, and selectively inhibits the neddylation modification of cullin 3 relative to other cullins. DI-1859 inactivates CRL3, promotes the accumulation of NRF2 and SLC7A11, upregulates the expression of HO-1 and NQO1, reduces reactive oxygen species (ROS) levels, enhances insulin signaling, promotes insulin secretion, activates RhoA, regulates the phosphorylation of AKT, without completely blocking the neddylation modification of cullin 3 or restoring the expression of IRS-1. DI-1859 can be used in the research of Acetaminophen (HY-66005)-induced hepatotoxicity, hyperglycemia, metabolic dysfunction-associated steatotic liver disease, insulin resistance, breast cancer and lung cancer .
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1 Cited Publications
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DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members .
Cat. No.: HY-W264347
CAS No.: 26028-65-9
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DCN1-UBC12-IN-4 (compound 5p) is an inhibitor of DCN1-UBC12, with an IC50 greater than 10000 nM, and it exhibits anti-tumor activity .
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WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
Cat. No.: HY-156240
CAS No.: 2247060-97-3
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DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
Cat. No.: HY-122874
CAS No.: 2187412-79-7
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DI-404 is a potent inhibitor of DCN1 with a KKd value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner .
Cat. No.: HY-161470
CAS No.: 2247544-03-0
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WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
Cat. No.: HY-169026
CAS No.: 2543578-57-8
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DCN1-IN-2 is a DCN1 inhibitor with an IC50 value of 2.96 nM. DCN1-IN-2 can alleviate Ang II/TGFβ-induced activation of cardiac fibroblasts. DCN1-IN-2 can reduce ISO-induced cardiac fibrosis and remodeling in mice by selectively inhibiting cullin 3 .
Cat. No.: HY-142694
CAS No.: 2374827-47-9
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DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
Cat. No.: HY-142691
CAS No.: 2374827-31-1
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DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect .
Cat. No.: HY-142692
CAS No.: 2374827-45-7
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DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect .
Cat. No.: HY-111505A
CAS No.: 2416146-10-4
NAcM-OPT (hydrochloride) is a protein interaction inhibitor. NAcM-OPT (hydrochloride) can disrupt the interaction between DCN1 and UBC12, with an IC50 value of 80 nM. NAcM-OPT (hydrochloride) can protect keratinocytes from H2O2-induced cell damage by promoting autophagy .
Cat. No.: HY-126075
CAS No.: 2247543-65-1
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WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
Cat. No.: HY-111505R
CAS No.: 2089293-61-6
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NAcM-OPT (Standard) is the analytical standard of NAcM-OPT (HY-111505). This product is intended for research and analytical applications. NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .
Cat. No.: HY-189074
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JN210 is a dual inhibitor of DCN1 and HDAC, with an IC50 of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer .
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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
