E1/E2/E3 Enzyme
E1 activating enzyme; E2 conjugating enzyme; E3 ligating enzyme; Ubiquitin activating enzyme; Ubiquitin conjugating enzyme; Ubiquitin ligase
Ubiquitin (UB) is a protein modifier that regulates many essential cellular processes. To initiate protein modification by UB, the E1 enzyme activates the C-terminal carboxylate of UB to launch its transfer through the E1-E2-E3 cascade onto target proteins. The E1 enzyme is the activating enzyme, to which ubiquitin is attached in an ATP-dependent reaction by a thioester bond. The E2 enzyme is the conjugating enzyme, to which the ubiquitin is transferred from the E1. The E3 is the ubiquitin ligase, which directly or indirectly catalyzes the transfer of the ubiquitin to the target protein (the substrate), with the formation of an isopeptide bond.
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E1/E2/E3 Enzyme Inhibitors
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E1/E2/E3 Enzyme Agonists
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E1/E2/E3 Enzyme Antagonist
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E1/E2/E3 Enzyme Activators
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E1/E2/E3 Enzyme Modulators
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E1/E2/E3 Enzyme Inducer
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E1/E2/E3 Enzyme Degraders
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E1/E2/E3 Enzyme Control
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E1/E2/E3 Enzyme Ligands
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Ubiquitin Enzymes Proteins
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E1/E2/E3 Enzyme Related Products (319)
Related Products (319)
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Recombinant Proteins (116)
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Antibodies (88)
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Related Compound Screening Libraries (1)
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Serdemetan
0 ImagesSynonyms: JNJ-26854165Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes.
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GS143
0 ImagesGS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
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SPOP-IN-6b
0 ImagesSPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM (patent CN 107141287, SPOP-B-88).
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HA-9104
0 ImagesHA-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.
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CP26
0 ImagesCP26 is a small molecule inhibitor of protein dislocation from the ER lumen to the cytosol. CP26 targets the Hrd1 complex, inhibits ERAD, and induces ER stress.
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BRD5529
0 ImagesBRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).
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HGC652
0 ImagesHGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death.
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Solasodine
0 ImagesSynonyms: Purapuridine; Solancarpidine; SolasodinSolasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2 proteins. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
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Anti-Mouse RANKL/CD254 Antibody (IK22/5)
0 ImagesCat. No.: HY-P990165Purity: 99.37%Anti-Mouse RANKL/CD254 Antibody (IK22/5) is an anti-mouse RANKL/CD254 IgG2a monoclonal antibody. Anti-Mouse RANKL/CD254 Antibody (IK22/5) inhibits osteoclast formation and activity by specifically blocking the binding of RANKL and RANK. Anti-Mouse RANKL/CD254 Antibody (IK22/5) can inhibit the expression of MuRF1/Trogin-1 and activation of NF-κB. Anti-Mouse RANKL/CD254 Antibody (IK22/5) can be used for research on cancer such as melanoma or colon cancer and osteoporosis.
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DI-591
0 ImagesDI-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.
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Cbl-b-IN-1
0 ImagesCbl-b-IN-1 (Example 519) is an inhibitor of Cbl-b, with an IC50 of less than 100 nM. Cbl-b-IN-1 can promote the secretion of cytokines such as IL-2, IFN-γ, and TNF-α, facilitate T cell activation, and enhance the TCR signaling pathway. Cbl-b-IN-1 can be used in research on immunomodulation.
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VHL-IN-1
0 ImagesVHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research.
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N106
0 ImagesN106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research.
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Ubiquitination-IN-1
0 ImagesUbiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
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UBE2T/FANCL-IN-1
0 ImagesUBE2T/FANCL-IN-1 is a potent inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, Carboplatin.
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1-Benzyl-I3C
0 Images1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1.
