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E1/E2/E3 Enzyme

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.

Ubiquitin-activating enzyme E1/Ubiquitin-conjugating enzyme E2/Ubiquitin ligase E3 (6)
产品名称 目录号 简述
CC0651 HY-15301

CC0651 是一种人Cdc34泛素结合酶变构抑制剂。CC0651 有效抑制 p27Kip1的泛素化,IC50 为 1.72 μM。

DKM 2-93 HY-101836

DKM 2-93是相对选择性的UBA5抑制剂,IC50值为430 μM。

PRT4165 HY-19817

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

PYR-41 HY-13296

PYR-41 是一种特异的,细胞可透过的 E1 抑制剂,IC50 值 < 10 μM。

PYZD-4409 HY-13297

PYZD-4409是泛素激活酶E1抑制剂,IC50为20 uM。

TZ9 HY-18643

TZ9是泛素结合酶(E2 enzyme)Rad6新型抑制剂,抑制MDA-MB-231细胞增殖的IC50值约为6uM。

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