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.

Cat. No.	製品名	CAS No.	Purity
T6629	PYR-41	418805-02-4	98%
T6629	PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
T4253	Skp2 Inhibitor C1	432001-69-9	98%
T4253	Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
T16699	PYZD-4409	423148-78-1	98%
T16699	PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells...
T14569	BI8626	1875036-75-1	98%
T14569	BI8626 is a ubiquitin ligase HUWE1 inhibitor with protective effects against spontaneous desiccation syndrome in NOD/ShiLtj mice.BI8626 inhibits intracellular ch...
T16974	TAK-243	1450833-55-2	98%
T16974	TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signa...
T6965	RG7112	939981-39-2
T6965	RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
T6S2123	Ginkgolic Acid	22910-60-7
T6S2123	Ginkgolic Acid (Romanicardic acid) C15:1 represses curli genes and prophage genes in EHEC.
T11980	MD-224	2136247-12-4	100%
T11980	MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
T2947	Indole-3-carbinol	700-06-1	100%
T2947	Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activatio...
T7889	C25-140	1358099-18-9	100%
T7889	C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T5199	COH000	1534358-79-6	96.91%
T5199	COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
T2243	Serdemetan	881202-45-5	97.13%
T2243	Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T9500	M435-1279	1359431-16-5	97.16%
T9500	M435-1279 is a UBE2T inhibitor. M435-1279 blocks UBE2T-mediated degradation of RACK1, leading to inhibit the hyperactivation of Wnt/β-catenin signaling pathway.
T10703	Mezigdomide	2259648-80-9	97.21%
T10703	Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that often acts as a molecular glue. Mezigdomide ...
T3653	MX69	1005264-47-0	97.27%
T3653	MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
T12261	NSC232003	1905453-18-0	97.72%
T12261	NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T7379	2-D08	144707-18-6	98%
T7379	2-D08 is a synthetic flavone that inhibits sumoylation, also inhibits Axl with an IC50 of 0.49 nM.2-D08 showed anti-aggregatory and neuroprotective effect.
T5555	Siremadlin	1448867-41-1	98.04%
T5555	Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T6585	SAR405838	1303607-60-4	98.04%
T6585	MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T13090	TAS4464 hydrochloride	1848959-11-4	98.18%
T13090	TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).