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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.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T4S0181 Hinokiflavone 19202-36-9 98.67%
Hinokiflavone
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...
T7415 DKM 2-93 65836-72-8 98.43%
DKM 2-93
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T16102 ML-792 1644342-14-2 98.22%
ML-792
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%
Subasumstat
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%
BH3I-1
BH3I-1 (BHI1) is a Bcl-2 antagonist.
T13090 TAS4464 hydrochloride 1848959-11-4 98.18%
TAS4464 hydrochloride
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%
SAR405838
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T7379 2-D08 144707-18-6 98%
2-D08
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 97.77%
Siremadlin
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T12261 NSC232003 1905453-18-0 97.72%
NSC232003
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T3653 MX69 1005264-47-0 97.27%
MX69
MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
T10703 Mezigdomide 2259648-80-9 97.21%
Mezigdomide
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%
M435-1279
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%
Serdemetan
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T5199 COH000 1534358-79-6 96.91%
COH000
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%
C25-140
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T3317 SZL P1-41 222716-34-9 100%
SZL P1-41
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...
T2947 Indole-3-carbinol 700-06-1 100%
Indole-3-carbinol
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%
MD-224
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.
T16974 TAK-243 1450833-55-2 98%
TAK-243
TAK-243 (MLN7243) is a small molecule inhibitor of ubiquitin-activating enzyme (UAE ,IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin sig...
Hinokiflavone
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...
DKM 2-93
T7415
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
ML-792
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...
Subasumstat
T8428
Subasumstat (TAK-981) is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
BH3I-1
T1493
BH3I-1 (BHI1) is a Bcl-2 antagonist.
TAS4464 hydrochloride
T13090
TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
SAR405838
T6585
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
2-D08
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.
Siremadlin
T5555
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
NSC232003
T12261
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
MX69
T3653
MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
Mezigdomide
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 ...
M435-1279
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.
Serdemetan
T2243
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
COH000
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).
C25-140
T7889
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
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...
Indole-3-carbinol
T2947
Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activatio...
MD-224
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.
TAK-243
T16974
TAK-243 (MLN7243) is a small molecule inhibitor of ubiquitin-activating enzyme (UAE ,IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin sig...
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