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-178517
    Thalidomide-C1-O-CO-C11
    Thalidomide-C1-O-CO-C11 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C11 can be connected to Aurora-A ligand 1 (HY-168440) by a linker (HY-178512) to form PROTAC CDK4/6/9 degrader 2 (HY-178516).
    Thalidomide-C1-O-CO-C11
  • HY-122615A
    SPOP-IN-6b hydrochloride
    		Inhibitor
    SPOP-IN-6b hydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
    SPOP-IN-6b hydrochloride
  • HY-W854844B
    JP-2-196 hydrochloride
    		Degrader
    JP-2-196 hydrochloride is a covalent molecular glue degrader targeting RNF126. JP-2-196 hydrochloride induces the formation of a ternary complex between RNF126 and target proteins (e.g., BRD4, AR-V7), promoting their ubiquitination and proteasomal degradation. JP-2-196 hydrochloride is promising for research of cancers (e.g., prostate cancer, leukemia).
    JP-2-196 hydrochloride
  • HY-175247
    DDO-4033
    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-156240
    DI-1548
    		Inhibitor
    DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research.
    DI-1548
  • HY-158172
    Cbl-b-IN-18
    		Inhibitor
    Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ligase Casitas B-lineage lymphoma proto-oncogene B (CPL-B). Cbl-b-IN-18 inhibits the phosphorylation of CPL-B (IC50< 100 nM).
    Cbl-b-IN-18
  • HY-122874
    DI-404
    		Inhibitor
    DI-404 is a potent inhibitor of DCN1 with a KKd value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner.
    DI-404
  • HY-145452
    5-Octyl-α-ketoglutarate
    		Inhibitor
    5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
    5-Octyl-α-ketoglutarate
  • HY-169796
    Panepophenanthrin
    		Inhibitor
    Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a ubiquitin-activating enzyme inhibitor.
    Panepophenanthrin
  • HY-W751400
    Solasodine hydrochloride
    		Inhibitor
    Solasodine (Purapuridine) hydrochloride is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine hydrochloride induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2 proteins. Solasodine hydrochloride has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
    Solasodine hydrochloride
  • HY-138165
    Ac-Phe-NH2
    Ac-Phe-NH2 is a non-competitive inhibitor of polyubiquitin chain elongation at Ki value of 8 mM by destabilizing the active trimer.
    Ac-Phe-NH2
  • HY-100507R
    Avadomide (Standard)
    		Agonist
    Avadomide (Standard) is the analytical standard of Avadomide. This product is intended for research and analytical applications. Avadomide is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities.
    Avadomide (Standard)
  • HY-18327
    HLI98C
    		Inhibitor
    HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation.
    HLI98C
  • HY-50696R
    Nutlin-3 (Standard)
    		Inhibitor
    Nutlin-3 (Standard) is the analytical standard of Nutlin-3. This product is intended for research and analytical applications. Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
    Nutlin-3 (Standard)
  • HY-N2360R
    Hinokiflavone (Standard)
    		Inhibitor
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.
    Hinokiflavone (Standard)
  • HY-141432G
    NX-1607 (GMP)
    		Inhibitor
    NX-1607 (Cbl-b-IN-3) (GMP) is a GMP-grade NX-1607 (HY-141432). GMP-grade small molecules can be used as adjuvant agents in cell therapy. NX-1607 (GMP) enhances antigen recall, reduces T cell exhaustion and increases cytokine production. NX-1607 is an inhibitor of Cbl-b (an E3 enzyme).
    NX-1607 (GMP)
  • HY-15676R
    Idasanutlin (Standard)
    		Inhibitor
    Idasanutlin (Standard) is the analytical standard of Idasanutlin. This product is intended for research and analytical applications. Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
    Idasanutlin (Standard)
  • HY-10029A
    (Rac)-Nutlin-3
    		Inhibitor
    (Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas.
    (Rac)-Nutlin-3
  • HY-70028
    p53 and MDM2 proteins-interaction-inhibitor (racemic)
    		Inhibitor
    p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor (racemic)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity