2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. E1/E2/E3 Enzyme

E1/E2/E3 Enzyme

E1 activating enzyme; E2 conjugating enzyme; E3 ligating enzyme; Ubiquitin activating enzyme; Ubiquitin conjugating enzyme; Ubiquitin ligase

E1/E2/E3 Enzyme

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W1128879
    XMU-MP-8
    		Degrader 99.23%
    XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma.
    XMU-MP-8
  • HY-110261
    GS143
    		Inhibitor 99.09%
    GS143 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.
    GS143
  • HY-122615
    SPOP-IN-6b
    		99.56%
    SPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM (patent CN 107141287, SPOP-B-88).
    SPOP-IN-6b
  • HY-160799
    HA-9104
    		98.54%
    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-115497
    BRD5529
    		Inhibitor 98.94%
    BRD5529 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).
    BRD5529
  • HY-170430
    HGC652
    		Ligand 98.86%
    HGC652 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.
    HGC652
  • HY-124602
    DI-591
    		Inhibitor 98.36%
    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-N0068
    Solasodine
    		Inhibitor 99.97%
    Solasodine (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.
    Solasodine
  • HY-P990165
    Anti-Mouse RANKL/CD254 Antibody (IK22/5)
    		Inhibitor 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.
    Anti-Mouse RANKL/CD254 Antibody (IK22/5)
  • HY-49116
    CP26
    		Inhibitor 98.19%
    CP26 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.
    CP26
  • HY-136339
    Cbl-b-IN-1
    		Inhibitor 99.66%
    Cbl-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.
    Cbl-b-IN-1
  • HY-120204
    BI8626
    		Inhibitor 98.49%
    BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM.
    BI8626
  • HY-156106
    VHL-IN-1
    		Inhibitor 99.84%
    VHL-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.
    VHL-IN-1
  • HY-110273
    N106
    		Activator 99.58%
    N106 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.
    N106
  • HY-135199
    Ubiquitination-IN-1
    		Inhibitor 99.43%
    Ubiquitination-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.
    Ubiquitination-IN-1
  • HY-115715
    EN219
    		99.21%
    EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination.
    EN219
  • HY-134656
    BC1618
    		99.74%
    BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
    BC1618
  • HY-141891
    M435-1279
    		Inhibitor 98.43%
    M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
    M435-1279
  • HY-126539
    UBE2T/FANCL-IN-1
    		99.36%
    UBE2T/FANCL-IN-1 is a potent inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, Carboplatin.
    UBE2T/FANCL-IN-1
  • HY-124586
    Streptonigrin
    		Inhibitor 99.20%
    Streptonigrin (Bruneomycin) is an orally active antibiotic and pan-PAD inhibitor, inhibiting PAD1, PAD2, PAD3 and PAD4 with IC50 of 48.3 μM, 26.1 μM, 0.43 μM and 2.5 μM, respectively. Streptonigrin inhibits SENP1 (IC50 of 0.518 μM) and reduces HIF1α. Streptonigrin increases p53 and Apoptosis. Streptonigrin shows antiviral activity against Rauscher murine leukemia virus. Streptonigrin has immunosuppressive effects. Streptonigrin has antitumor activity against osteosarcoma.
    Streptonigrin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity