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-156765
    Cbl-b-IN-9
    		Inhibitor 98.55%
    Cbl-b-IN-9 (Compound 300) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.6 nM and 4.7 nM, respectively.
    Cbl-b-IN-9
  • HY-167673
    RNF5-IN-1
    		Degrader 98.52%
    RNF5-IN-1 (FX12) is a selective RNF5 degrader. RNF5-IN-1 binds to RNF5 and inhibits its E3 activity, and promotes proteasomal degradation of RNF5 in an endoplasmic reticulum (ER)-associated degradation (ERAD) way in cells. RNF5-IN-1 inhibits α-1-antitrypsin (NHK) dislocation with an IC50 value of 2.7 μM. RNF5-IN-1 can be used for research of cystic fibrosis, acute myeloid leukemia, and certain viral infections.
    RNF5-IN-1
  • HY-70027A
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride
    		Inhibitor 99.56%
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride
  • HY-101266B
    Milademetan tosylate hydrate
    		Inhibitor 98.89%
    Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
    Milademetan tosylate hydrate
  • HY-109045A
    Teslexivir hydrochloride
    		Inhibitor 98.28%
    Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.
    Teslexivir hydrochloride
  • HY-P3709A
    TRAF6 peptide TFA
    		Inhibitor 98.20%
    TRAF6 peptide TFA is a specific TRAF6-p62 inhibitor. TRAF6 peptide TFA potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide TFA has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
    TRAF6 peptide TFA
  • HY-163518
    Antitumor agent-153
    		99.62%
    Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity.
    Antitumor agent-153
  • HY-W062696
    BC-1382
    		Inhibitor 99.36%
    BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
    BC-1382
  • HY-156766
    Cbl-b-IN-10
    		Inhibitor 98.85%
    Cbl-b-IN-10 is a Cbl-b and c-Cbl inhibitor with IC50 values of 6.0 nM and 3.5 nM, respectively. Cbl-b-IN-10 can be used in the study of cancer.
    Cbl-b-IN-10
  • HY-W340839
    p53-MDM2-IN-1
    		Inhibitor 99.91%
    p53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an Ki value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research.
    p53-MDM2-IN-1
  • HY-156769
    Cbl-b-IN-13
    		Inhibitor 98.46%
    Cbl-b-IN-13 (Example 520) is a Cbl-b inhibitor with an IC50 of <100 nM. Cbl-b-IN-13 has the ability to activate T-cells.
    Cbl-b-IN-13
  • HY-175247
    DDO-4033
    		99.11%
    DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.
    DDO-4033
  • HY-N0170R
    Indole-3-carbinol (Standard)
    		Inhibitor
    Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
    Indole-3-carbinol (Standard)
  • HY-15954B
    NVP-CGM097 sulfate
    		Inhibitor 98.82%
    NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
    NVP-CGM097 sulfate
  • HY-182467
    BMS-986482
    BMS-986482 is a CELMoD, CRBN-mediated, selective IKZF1-4 Molecular Glue degrader. The activity of BMS-986482 is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 inhibits tumor growth in preclinical mouse models. BMS-986482 can be used for the research of advanced solid tumors. .
    BMS-986482
  • HY-181692
    PROTAC RNF4 degrader-1
    		Degrader
    PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
    PROTAC RNF4 degrader-1
  • HY-141431
    Cbl-b-IN-2
    		Inhibitor
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
    Cbl-b-IN-2
  • HY-125858A
    MI-1061 TFA
    		Inhibitor
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    MI-1061 TFA
  • HY-156768
    Cbl-b-IN-12
    		Inhibitor
    Cbl-b-IN-12 (Example 10) is a casitas B-lineage lymphoma-b (CBL-B) inhibitor with an IC50 of <100 nM.
    Cbl-b-IN-12
  • HY-175187
    LO-3-63
    		98.16%
    LO-3-63, a Ribociclib (HY-15777) analog bearing a truncated fumaramide handle, is a PROTAC-like CDK4/6 degrader. LO-3-63 induces CUL4DCAF16-dependent degradation of CDK4/6 in cells.
    LO-3-63
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Cat. No. Product Name / Synonyms Application Reactivity