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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
T16699 PYZD-4409 PYZD-4409 是一种特异性 UBA1 抑制剂,IC50 为 20 μM。 PYZD-4409 在恶性细胞中诱导细胞死亡,并且对恶性细胞的细胞毒性优于对正常造血细胞的细胞毒性。
T24136 Heclin Heclin 是一种 HECT E3 泛素连接酶抑制剂,通过抑制 Smurf2、Nedd4 和 WWP1 起作用,IC50 值分别为 6.8、6.3 和 6.9 μM。
T16901 SMIP004 SMIP004 是一种 SKP2 E3 连接酶抑制剂。 SMIP004 是人前列腺癌细胞的癌细胞特异性凋亡诱导剂。
T13090 TAS4464 hydrochloride TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
T4S0181 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...
T6254 Idasanutlin Idasanutlin (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
T5555 Siremadlin Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T7889 C25-140 C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T4253 Skp2 Inhibitor C1 Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
T6332 Pevonedistat MLN4924 is an effective and specific small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50: 4.7 nM).
T3549 Avadomide CC-122 is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
T8564 BC-1382 BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
T6629 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
T9236 WSB1 Degrader 1 WSB1 Degrader 1 is a poten and orally active WD repeat and SOCS box-containing 1 degrader. WSB1 Degrader 1 has anticancer metastatic effects
T8816 NAE-IN-M22 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...
T16102 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...
T6614 Nutlin-3b Nutlin-3b is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nu...
T6023 Nutlin-3a Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
T3517 RO8994 RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding ...
T2158 Nutlin-3 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...
T6585 SAR405838 MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T6S2123 Ginkgolic Acid 1. Ginkgolic acid C15:1 represses curli genes and prophage genes in EHEC.
T11980 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.
T25465 GS143 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 NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
T3317 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...
T3110 PRT4165 PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.
TQ0127 Navtemadlin 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.
T3653 MX69 MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
T12261 NSC232003 NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T16888 SJ-172550 SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
T6149 YH239-EE YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T4036 Solasodine Solasodine(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity again...
T2243 Serdemetan Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T1493 BH3I-1 BH3I-1 is a Bcl-2 antagonist.
T2947 Indole-3-carbinol Indole-3-carbinol, a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
T10703 Mezigdomide CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD) with potent antimyeloma activity.
T6965 RG7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
T6611 NSC697923 NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
T7379 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.
T7415 DKM 2-93 DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T8428 Subasumstat TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
T8929 BC1618 BC1618 is an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling. It promotes mitochondrial fission, facilitates autophagy and improves...
T13090L TAS4464 TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
TQ0231 NVP-CGM097 NVP-CGM097 is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
T5199 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).
T13349 WS-383 WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).
T16974 TAK-243 TAK-243 is a small molecule inhibitor of ubiquitin-activating enzyme (UAE ,IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as ...
PYZD-4409
T16699
Heclin
T24136
Heclin 是一种 HECT E3 泛素连接酶抑制剂,通过抑制 Smurf2、Nedd4 和 WWP1 起作用,IC50 值分别为 6.8、6.3 和 6.9 μM。
SMIP004
T16901
SMIP004 是一种 SKP2 E3 连接酶抑制剂。 SMIP004 是人前列腺癌细胞的癌细胞特异性凋亡诱导剂。
TAS4464 hydrochloride
T13090
TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
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...
Idasanutlin
T6254
Idasanutlin (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
Siremadlin
T5555
Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
C25-140
T7889
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
Skp2 Inhibitor C1
T4253
Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
Pevonedistat
T6332
MLN4924 is an effective and specific small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50: 4.7 nM).
Avadomide
T3549
CC-122 is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
BC-1382
T8564
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
PYR-41
T6629
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
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
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...
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 ...
Nutlin-3b
T6614
Nutlin-3b is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer N...
Nutlin-3a
T6023
Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
RO8994
T3517
RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding ...
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; i...
SAR405838
T6585
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Ginkgolic Acid
T6S2123
1. Ginkgolic acid C15:1 represses curli genes and prophage genes in EHEC.
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.
GS143
T25465
NAcM-OPT
T5374
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
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...
PRT4165
T3110
PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.
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.
MX69
T3653
MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
NSC232003
T12261
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
SJ-172550
T16888
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
YH239-EE
T6149
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
Solasodine
T4036
Solasodine(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity again...
Serdemetan
T2243
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
BH3I-1
T1493
BH3I-1 is a Bcl-2 antagonist.
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.
RG7112
T6965
RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
NSC697923
T6611
NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
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.
DKM 2-93
T7415
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
Subasumstat
T8428
TAK-981 is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
BC1618
T8929
BC1618 is an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling. It promotes mitochondrial fission, facilitates autophagy and improves...
TAS4464
T13090L
TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
NVP-CGM097
TQ0231
NVP-CGM097 is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
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).
WS-383
T13349
WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).
TAK-243
T16974
TAK-243 is a small molecule inhibitor of ubiquitin-activating enzyme (UAE ,IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as ...