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
T63790	Cbl-b-IN-3	2573775-59-2	98%
T63790	Cbl-b-IN-3 is a potent proto-oncogene-B (CPL-B) inhibitor of casitas B-series lymphoma (ic50 < 1 nM). Cpl-b, a cyclic E3 ubiquitin protein ligase, is involved in...
TQ0127	Navtemadlin	1352066-68-2	98%
TQ0127	AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
T5374	NAcM-OPT	2089293-61-6	98%
T5374	NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 （IC50: 79 nM).
T6585	SAR405838	1303607-60-4	98%
T6585	MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T9500	M435-1279	1359431-16-5	98%
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.
T16102	ML-792	1644342-14-2	98%
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...
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...
T16901	SMIP004	143360-00-3	98%
T16901	SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
T12261	NSC232003	1905453-18-0
T12261	NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T5555	Siremadlin	1448867-41-1
T5555	Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T8428	Subasumstat	1858276-04-6
T8428	TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
T6149	YH239-EE	1364488-67-4	100%
T6149	YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
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.
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).
T2947	Indole-3-carbinol	700-06-1	97.06%
T2947	Indole-3-carbinol, a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
T10703	Mezigdomide	2259648-80-9	97.21%
T10703	CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD) with potent antimyeloma activity.
T2243	Serdemetan	881202-45-5	98%
T2243	Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
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.
T1493	BH3I-1	300817-68-9	98.2%
T1493	BH3I-1 is a Bcl-2 antagonist.