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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.
Cat. No. Product name CAS No. Purity Chemical Structure
T13090L TAS4464 1848959-10-3 98%
TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
T2158 Nutlin-3 548472-68-0 98%
Nutlin-3 is an MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; in...
T16888 SJ-172550 431979-47-4 98%
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
T3317 SZL P1-41 222716-34-9 98%
SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the act...
T25465 GS143 916232-21-8 98%
GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and t...
T5374 NAcM-OPT 2089293-61-6 98%
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
T13412 ZM223 2031177-48-5 98%
ZM223 is an inhibitor of NEDD8 activating enzyme (NAE).
T9236 WSB1 Degrader 1 2306039-66-5 98%
WSB1 Degrader 1 is a poten and orally active WD repeat and SOCS box-containing 1 degrader. WSB1 Degrader 1 has anticancer metastatic effects
T4036 Solasodine 126-17-0 98%
Solasodine(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity again...
T16901 SMIP004 143360-00-3 98%
SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
T6149 YH239-EE 1364488-67-4 98%
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T3110 PRT4165 31083-55-3 98%
PRT4165 is a potent PRC1-mediated H2A ubiquitylation inhibitor.
T6254 Idasanutlin 1229705-06-9 98%
Idasanutlin (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
T72043 SCFSkp2-IN-2 1375060-02-8 98%
SCFSkp2-IN-2 is a Skp2 inhibitor with a K D of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities .
T24136 Heclin 890605-54-6 98%
Heclin is an inhibitor of HECT E3 ubiquitin ligase that acts by inhibiting Smurf2, Nedd4, and WWP1 with IC50 values of 6.8, 6.3, and 6.9 μM, respectively.
T6332 Pevonedistat 905579-51-3 98%
MLN4924 is an effective and specific small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50: 4.7 nM).
T8564 BC-1382 1013753-99-5 98%
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
T8929 BC1618 2222094-18-8 98%
BC1618 is an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling. It promotes mitochondrial fission, facilitates autophagy and improves...
T3549 Avadomide 1015474-32-4 98%
CC-122 is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
T63790 Cbl-b-IN-3 2573775-59-2 98%
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...
TAS4464
T13090L
TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
Nutlin-3
T2158
Nutlin-3 is an MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; in...
SJ-172550
T16888
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
SZL P1-41
T3317
SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the act...
GS143
T25465
GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and t...
NAcM-OPT
T5374
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
ZM223
T13412
ZM223 is an inhibitor of NEDD8 activating enzyme (NAE).
WSB1 Degrader 1
T9236
WSB1 Degrader 1 is a poten and orally active WD repeat and SOCS box-containing 1 degrader. WSB1 Degrader 1 has anticancer metastatic effects
Solasodine
T4036
Solasodine(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity again...
SMIP004
T16901
SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
YH239-EE
T6149
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
PRT4165
T3110
PRT4165 is a potent PRC1-mediated H2A ubiquitylation inhibitor.
Idasanutlin
T6254
Idasanutlin (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
SCFSkp2-IN-2
T72043
SCFSkp2-IN-2 is a Skp2 inhibitor with a K D of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities .
Heclin
T24136
Heclin is an inhibitor of HECT E3 ubiquitin ligase that acts by inhibiting Smurf2, Nedd4, and WWP1 with IC50 values of 6.8, 6.3, and 6.9 μM, respectively.
Pevonedistat
T6332
MLN4924 is an effective and specific small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50: 4.7 nM).
BC-1382
T8564
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
BC1618
T8929
BC1618 is an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling. It promotes mitochondrial fission, facilitates autophagy and improves...
Avadomide
T3549
CC-122 is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
Cbl-b-IN-3
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...
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