Signaling Pathway

E1/E2/E3 Enzyme

E1/E2/E3 Enzyme

Related Products

PDF File 0.22MB

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 Inhibitors & Modulators (6)

Product Name Catalog No. Brief Description
CC0651

HY-15301

CC0651 is an allosteric inhibitor of the human cdc34 ubiquitin-conjugating enzyme that potently (IC50 = 1.72 uM) inhibited the ubiquitination of p27 Kip1.

CC122

HY-100507

CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity.

PRT4165

HY-19817

PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.

PYR-41

HY-13296

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 uM, with no or little activity at E2.

PYZD-4409

HY-13297

PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay).

TZ9

HY-18643

TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.