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Results for "

cullin neddylation

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-160799
    HA-9104
    1 Publications Verification

    		 E1/E2/E3 Enzyme Apoptosis Cancer
    HA-9104 is a potent and selective inhibitor of cullin-5 neddylation via virtually targeting the V30 pocket of UBE2F. HA-9104 binds to UBE2F, reduces its protein levels, and consequently inhibits cullin-5 neddylation. HA-9104 has potent growth suppression and radiosensitizing activities via targeting the UBE2F-CRL5 axis and causing DNA damage, leading to induction of apoptosis and G2/M arrest in lung and pancreatic cancer cells .
    HA-9104
  • HY-124602
    DI-591

    		E1/E2/E3 Enzyme Cancer
    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 .
    DI-591
  • HY-111505
    NAcM-OPT
    2 Publications Verification

    		 E1/E2/E3 Enzyme NEDD8-activating Enzyme Cancer
    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .
    NAcM-OPT
  • HY-128586A
    TAS4464 hydrochloride
    Maximum Cited Publications
    9 Publications Verification

    		 NEDD8-activating Enzyme Carbonic Anhydrase Apoptosis Cancer
    TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
    TAS4464 hydrochloride
  • HY-145733
    DI-1859

    		E1/E2/E3 Enzyme Cardiovascular Disease
    DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage .
    DI-1859
  • HY-156240
    DI-1548

    		E1/E2/E3 Enzyme Keap1-Nrf2 Metabolic Disease
    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 .
    DI-1548
  • HY-162240
    SJH1-51B

    		PROTACs Epigenetic Reader Domain Cancer
    SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research .
    SJH1-51B
  • HY-122874
    DI-404

    		E1/E2/E3 Enzyme Cardiovascular Disease
    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 .
    DI-404
  • HY-172252
    CSN5-IN-2

    		PD-1/PD-L1 RAD51 Cancer
    CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. CSN5-IN-2 can increase the level of Cullin 1 neddylation, and downregulate the expression of RAD51 and PD-L1 in cancer cells. CSN5-IN-2 has anti-tumor activity, and its effect is better when combined with Talazoparib (HY-16106) .
    CSN5-IN-2

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