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

Related Products

PDF 1.36 MB

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-136262
    CRBN-6-5-5-VHL
    		Degrader 99.45%
    CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)).
    CRBN-6-5-5-VHL
  • HY-15954
    NVP-CGM097
    		Inhibitor 98.08%
    NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
    NVP-CGM097
  • HY-148266
    UBA5-IN-1
    		Inhibitor 98.0%
    UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5.
    UBA5-IN-1
  • HY-148900
    SCFSkp2-IN-2
    		Inhibitor 99.01%
    SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.
    SCFSkp2-IN-2
  • HY-10949
    SMER3
    		Inhibitor 98.33%
    SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30.
    SMER3
  • HY-170430
    HGC652
    		Ligand 98.86%
    HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21.
    HGC652
  • HY-128845
    PROTAC CRBN Degrader-1
    		Degrader 99.84%
    PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other. (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
    PROTAC CRBN Degrader-1
  • 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-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
  • HY-15694
    SMIP004
    		Inhibitor 99.79%
    SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
    SMIP004
  • HY-139662
    HB007
    		Inhibitor 99.73%
    HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
    HB007
  • HY-125858
    MI-1061
    		Inhibitor 99.72%
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    MI-1061
  • HY-111505
    NAcM-OPT
    		Inhibitor 99.65%
    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.
    NAcM-OPT
  • HY-49444
    EN450
    		98.59%
    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
    EN450
  • HY-15335
    Nutlin-3b
    		Inhibitor 98.78%
    Nutlin-3b, the inactive form of Nutlin-3 (HY-50696), is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a (HY-10029). Nutlin-3b is promising for research of cancers.
    Nutlin-3b
  • HY-P990165
    Anti-Mouse RANKL/CD254 Antibody (IK22/5)
    		Inhibitor
    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-18643
    TZ9
    		Inhibitor 99.45%
    TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells.
    TZ9
  • HY-157435
    PELI1-IN-1
    		Inhibitor 98.02%
    PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.or effect.
    PELI1-IN-1
  • HY-123967
    RNF5 inhibitor inh-02
    		Inhibitor 99.91%
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 rescues F508del-CFTR function in F508del-CFTR-expressing immortalized cells (CFBE41o⁻, EC50 = 2.6 μM; FRT, EC 50 = 2.2 μM). RNF5 inhibitor inh-02 increases LC3IIB expression and autophagic vacuole number via reducing ATG4B ubiquitylation and promotes cell motility. RNF5 inhibitor inh-02 can be used for the study of cystic fibrosis.
    RNF5 inhibitor inh-02
  • HY-148602
    KH-4-43
    		Inhibitor 99.99%
    KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively.
    KH-4-43
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity