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
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...
T11980	MD-224	2136247-12-4	98%
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.
T6149	YH239-EE	1364488-67-4	98%
T6149	YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T7889	C25-140	1358099-18-9	98%
T7889	C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T5199	COH000	1534358-79-6	98%
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	98%
T2947	Indole-3-carbinol, a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
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.
T12261	NSC232003	1905453-18-0	98%
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%
T5555	Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T6585	SAR405838	1303607-60-4	98%
T6585	MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T13090	TAS4464 hydrochloride	1848959-11-4	98%
T13090	TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
T2243	Serdemetan	881202-45-5	98%
T2243	Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T1493	BH3I-1	300817-68-9	98%
T1493	BH3I-1 is a Bcl-2 antagonist.
T8428	Subasumstat	1858276-04-6	98%
T8428	TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
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...
T7415	DKM 2-93	65836-72-8	98%
T7415	DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T4S0181	Hinokiflavone	19202-36-9	98%
T4S0181	Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spli...
T8816	NAE-IN-M22	864420-54-2	98%
T8816	NAE-IN-M22 is a selective, potent and reversible inhibitor of NEDD8 activating enzyme (NAE). NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis...
T6023	Nutlin-3a	675576-98-4	98%
T6023	Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.