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 (320)
Related Products (320)
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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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MI-1061 TFA
0 ImagesCat. No.: HY-125858ACAS No.: 1410737-35-7
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Idasanutlin-d3-1
0 ImagesCat. No.: HY-153939SPurity: 99.57%Synonyms: RG7388-d3-1Idasanutlin-d3-1 (RG7388-d3-1) is the deuterated-labeled Idasanutlin (HY-15676). Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors.
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NVS1.1
0 ImagesCat. No.: HY-177569NVS1.1 is an orally active, blood-brain barrier-penetrant eRF1 degrader. NVS1.1 induces ubiquitination of eRF1 at Lys279, mediates proteasomal degradation via the E3 ubiquitin ligases RNF14 and RNF25 as well as the translational stress sensor GCN1, traps eRF1 at the ribosomal A-site, inhibits translation termination and triggers ribosome collision. As a readthrough enhancer, NVS1.1 enables near-cognate tRNA incorporation at premature termination codons by reducing intracellular eRF1 levels. NVS1.1 activates ribosome-associated quality control pathways via ribosome collision, including ubiquitination of small subunit ribosomal proteins. NVS1.1 restores functional full-length CFTR and IDUA proteins and reduces glycosaminoglycan accumulation in relevant models. NVS1.1 can be used in the research of cystic fibrosis and Hurler syndrome (mucopolysaccharidosis type I, MPS I).
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Cbl-b-IN-12
0 ImagesCat. No.: HY-156768CAS No.: 2851871-29-7Cbl-b-IN-12 (Example 10) is a casitas B-lineage lymphoma-b (CBL-B) inhibitor with an IC50 of <100 nM.
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H111-H7
0 ImagesH111-H7 is a WW domain containing E3 ubiquitin 27 protein ligase 2 (WWP2) inhibitor with a KD of 717 nM. H111-H7 inhibits WWP2 expression, restores the succinate dehydrogenase complex subunit C (SDHC) level, and defers the acute kidney injury (AKI)-to-chronic kidney disease (CKD) transition in unilateral kidney ischemia–reperfusion (UIR) mice. H111-H7 can be used for AKI-to-CKD transition research.
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JWZ-8-103
0 ImagesJWZ-8-103 is an orally active analog of PRLX-93936 (HY-119264) and a molecular glue targeting TRIM21. JWZ-8-103 increases the thermal stability of TRIM21. JWZ-8-103 promotes rapid and efficient interaction between TRIM21 and NUP98 (the apparent EC50 for ternary complex formation with the PRYSPRY domain of TRIM21 and the APD domain of NUP98 is approximately 20 μM), induces extensive ubiquitination and proteasomal degradation of numerous adjacent nucleoporins (NUPs, and thereby triggers cellular apoptosis. JWZ-8-103 can be used for the research of pancreatic cancer.
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SPI-05
0 ImagesCat. No.: HY-W342380CAS No.: 5463-64-9Synonyms: NSC 5067SPI-05 (NSC 5067) is a non-competitive SUMO-specific proteases (SENP1/2) inhibitor (IC50=60 μM). SPI-05 is promising for research of cancers, such as prostate cancer and hypoxia-driven solid tumors with SENP1 overexpression.
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Solasodine (Standard)
0 ImagesSynonyms: Purapuridine (Standard); Solancarpidine (Standard); Solasodin (Standard)Solasodine (Standard) is the analytical standard of Solasodine. This product is intended for research and analytical applications. Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
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WS-384
0 ImagesWS-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).
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Smurf1-IN-5
0 ImagesCat. No.: HY-174416CAS No.: 1824647-09-7Smurf1-IN-5 (Compound cpd-6) is an allosteric SMAD ubiquitin regulatory factor 1 (SMURF1) inhibitor. Smurf1-IN-5 leads to a reduction in the ubiquitylation of substrates such as BMPR2 (bone morphogenetic protein receptor 2) and SMAD1, enhancing the BMP (bone morphogenetic protein) signaling pathway. Smurf1-IN-5 is promising for research of pulmonary arterial hypertension (PAH).
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MRT-31619
0 ImagesCat. No.: HY-180538MRT-31619 is a selective CRBN Molecular glue degrader, with an IC50 of 14 nM and an EC50 of 72 nM. MRT-31619 triggers ubiquitination and proteasomal degradation of CRBN. MRT-31619 serves as a chemical knockout tool for CRBN depletion to evaluate the dependence of other molecular glues on CRBN. MRT-31619 is applicable to the research of CRBN-related disease models.
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ML307
0 ImagesML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research.
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H36-E4
0 ImagesH36-E4 is a WW domain containing E3 ubiquitin 27 protein ligase 2 (WWP2) inhibitor with a KD of 6.25 μM. H36-E4 inhibits WWP2 expression, restores the succinate dehydrogenase complex subunit C (SDHC) level, and defers the acute kidney injury (AKI)-to-chronic kidney disease (CKD) transition in unilateral kidney ischemia-reperfusion (UIR) mice. H36-E4 can be used for AKI-to-CKD transition research.
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BMS-986482 acetate
0 ImagesCat. No.: HY-182467APurity: 98.04%BMS-986482 acetate is a CRBN-mediated IKZF1-4 (Ikaros family zinc finger 1-4) molecular glue degrader. BMS-986482 acetate's activity is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 acetate can be used for the research of advanced solid tumors.
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T521
0 ImagesT521 is an inhibitor of E3 ligase. T521 can be used in cancer and metabolic disease related research.
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TRAF6 peptide
0 ImagesCat. No.: HY-P3709CAS No.: 852805-92-6TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
