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.

E1/E2/E3 Enzyme Related Products (154)
Recombinant Proteins (118)
Antibodies (86)

By Effects:	Inhibitors (134) Agonists (2) Degrader (1) Activators (3) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-N0077

Ginkgolic Acid	Inhibitor	99.92%
Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC₅₀ of 3.0 μM in in vitro assay.

HY-101266

Milademetan	Inhibitor	98.77%
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

HY-110204

Heclin	Inhibitor	98.21%
Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC₅₀ values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer.

HY-10959

RG7112	Inhibitor	99.91%
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2.

HY-136339

Cbl-b-IN-1	Inhibitor	99.68%
Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC₅₀ <100 nM.

HY-13811

NSC697923	Inhibitor	99.93%
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.

HY-19817

PRT4165	Inhibitor	≥98.0%
PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation.

HY-100237

SZL P1-41	Inhibitor	99.92%
SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.

HY-120929

BI8622	Inhibitor	98.28%
BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 3.1 μM.

HY-101518

Alrizomadlin	Inhibitor	98.67%
Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC₅₀ and K_i values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

HY-103236

NSC232003	Inhibitor	99.67%
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.

HY-100507

Avadomide	Agonist	99.14%
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.

HY-120204

BI8626	Inhibitor	99.20%
BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 0.9 μM.

HY-141432

NX-1607	Inhibitor	99.42%
NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC₅₀ value of less than 1 nM. NX-1607 can be used in cancer research.

HY-16661

Skp2 Inhibitor C1	Inhibitor	98.21%
Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis.

HY-101836

DKM 2-93	Inhibitor	98.76%
DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC₅₀ of 430 μM.

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).

HY-135199

Ubiquitination-IN-1	Inhibitor	99.84%
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.

HY-18986

SAR405838	Inhibitor	99.19%
SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a K_i of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity.

HY-152859

Brigimadlin	Inhibitor	99.72%
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research.

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E1/E2/E3 Enzyme

E1/E2/E3 Enzyme

E1/E2/E3 Enzyme Related Products (154)

Recombinant Proteins (118)

Antibodies (86)

E1/E2/E3 Enzyme Related Products (154):