Home Tools
Log in
Cart

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
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...
T11980 MD-224 2136247-12-4 98%
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%
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T7889 C25-140 1358099-18-9 98%
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T5199 COH000 1534358-79-6 98%
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%
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%
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%
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
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.
T5555 Siremadlin 1448867-41-1 98%
Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T6585 SAR405838 1303607-60-4 98%
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T13090 TAS4464 hydrochloride 1848959-11-4 98%
TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
T2243 Serdemetan 881202-45-5 98%
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T1493 BH3I-1 300817-68-9 98%
BH3I-1 is a Bcl-2 antagonist.
T8428 Subasumstat 1858276-04-6 98%
TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
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...
T7415 DKM 2-93 65836-72-8 98%
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T4S0181 Hinokiflavone 19202-36-9 98%
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%
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%
Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
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...
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.
YH239-EE
T6149
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
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.
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.
NSC232003
T12261
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
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 is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
SAR405838
T6585
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
TAS4464 hydrochloride
T13090
TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
Serdemetan
T2243
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
BH3I-1
T1493
BH3I-1 is a Bcl-2 antagonist.
Subasumstat
T8428
TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
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...
DKM 2-93
T7415
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
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...
NAE-IN-M22
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...
Nutlin-3a
T6023
Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
1 2 3