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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
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...
TQ0127 Navtemadlin 1352066-68-2 98%
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%
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
T6585 SAR405838 1303607-60-4 98%
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T9500 M435-1279 1359431-16-5 98%
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%
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%
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%
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
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T5555 Siremadlin 1448867-41-1
Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T8428 Subasumstat 1858276-04-6
TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
T6149 YH239-EE 1364488-67-4 100%
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T11980 MD-224 2136247-12-4 100%
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%
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T5199 COH000 1534358-79-6 96.91%
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%
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%
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD) with potent antimyeloma activity.
T2243 Serdemetan 881202-45-5 98%
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T7379 2-D08 144707-18-6 98%
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%
BH3I-1 is a Bcl-2 antagonist.
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...
Navtemadlin
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.
NAcM-OPT
T5374
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
SAR405838
T6585
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
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.
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...
PYZD-4409
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...
SMIP004
T16901
SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
NSC232003
T12261
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
Siremadlin
T5555
Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
Subasumstat
T8428
TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
YH239-EE
T6149
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
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.
C25-140
T7889
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
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).
Indole-3-carbinol
T2947
Indole-3-carbinol, a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
Mezigdomide
T10703
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD) with potent antimyeloma activity.
Serdemetan
T2243
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
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.
BH3I-1
T1493
BH3I-1 is a Bcl-2 antagonist.
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