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.	Product name	CAS No.	Purity
T6023	Nutlin-3a	675576-98-4	98.73%
T6023	Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
T8816	NAE-IN-M22	864420-54-2	98.67%
T8816	NAE-IN-M22 (NEDD8 inhibitor M22) is a selective, potent and reversible inhibitor of NEDD8 activating enzyme (NAE). NAE-IN-M22 inhibits multiple cancer cell lines...
T4S0181	Hinokiflavone	19202-36-9	98.67%
T4S0181	Hinokiflavone, a novel modulator of pre-mRNA splicing activity both in vitro and in cellulo, inhibits the assembly of the spliceosome, particularly blocking the ...
T7415	DKM 2-93	65836-72-8	98.43%
T7415	DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T16102	ML-792	1644342-14-2	98.22%
T16102	ML-792 is a specific small ubiquitin-like modifier (SUMO)-activating enzyme (SAE) inhibitor. Compared with NAE/NEDD8 and UAE/ubiquitin (IC50s of 32 μM and >100 μ...
T8428	Subasumstat	1858276-04-6	98.22%
T8428	Subasumstat (TAK-981) is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
T1493	BH3I-1	300817-68-9	98.2%
T1493	BH3I-1 (BHI1) is a Bcl-2 antagonist.
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).
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.
T5555	Siremadlin	1448867-41-1	98.04%
T5555	Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
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.
T12261	NSC232003	1905453-18-0	97.72%
T12261	NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
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.
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 ...
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.
T2243	Serdemetan	881202-45-5	97.13%
T2243	Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
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).
T7889	C25-140	1358099-18-9	100%
T7889	C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
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...
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.