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Search Result

Search Results for " e1-activating "

Targets

E1/E2/E3 Enzyme

43

Compounds

5

Natural Products

15

Recombinant Proteins

1

Libraries

Cat No. Product Name Synonyms Targets
T24136 Heclin E1/E2/E3 Enzyme
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.
T5374 NAcM-OPT E1/E2/E3 Enzyme , NEDD8
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 （IC50: 79 nM).
T16901 SMIP004 Apoptosis , Others , E1/E2/E3 Enzyme
SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
T3517 RO8994 Mdm2 , E1/E2/E3 Enzyme , p53
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 assays).
T8428 Subasumstat TAK-981 E1/E2/E3 Enzyme
Subasumstat (TAK-981) is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
T16102 ML-792 E1/E2/E3 Enzyme
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 μM, respectively), ML-792 is an effective and selective inhi...
T16699 PYZD-4409 Others , E1/E2/E3 Enzyme
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 over normal hematopoietic cells.
T5199 COH000 E1/E2/E3 Enzyme
COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
T13244 Ubiquitination-IN-1 Others
Ubiquitination-IN-1 is an inhibitor of ubiquitination and Cksl-Skp2 protein-protein interaction (IC50: 0.17 μM).
T12261 NSC232003 E1/E2/E3 Enzyme
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T7415 DKM 2-93 E1/E2/E3 Enzyme
DKM 2-93 is a relatively selective inhibitor of UBA5(IC50 : 430 μM).
T6629 PYR-41 PYR41,PYR 41 Apoptosis , E1/E2/E3 Enzyme
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
T2158 Nutlin-3 Nutlin3 E1/E2/E3 Enzyme
Nutlin-3 is an MDM2 antagonist.Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; induces apoptosis in Y cells.
T7379 2-D08 E1/E2/E3 Enzyme , TAM Receptor
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.
T16888 SJ-172550 Mdm2 , E1/E2/E3 Enzyme
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
T9236 WSB1 Degrader 1 Others , E1/E2/E3 Enzyme
WSB1 Degrader 1 is a potent, orally active degrader of WD repeat and SOCS box-containing 1, exhibiting anti-cancer metastatic effects.
T3653 MX69 Mdm2 , E1/E2/E3 Enzyme , IAP
MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
T6149 YH239-EE Apoptosis , E1/E2/E3 Enzyme
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
T3317 SZL P1-41 Apoptosis , Others , E1/E2/E3 Enzyme
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 activity of other SCF complexes. It also inhibits Skp2-mediate...
T4253 Skp2 Inhibitor C1 SKPin C1 Others , E1/E2/E3 Enzyme
Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
T11980 MD-224 Mdm2 , E1/E2/E3 Enzyme , PROTACs
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 Others , TNF , E1/E2/E3 Enzyme , NF-κB
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T10703 Mezigdomide CC-92480 Apoptosis , E1/E2/E3 Enzyme , Molecular Glues
Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that often acts as a molecular glue. Mezigdomide has antimyeloma activity.
T13349 WS-383 E1/E2/E3 Enzyme
WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).
T23371 SMER3 SMER 3 Others , Ligand for E3 Ligase
SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune respon...
T8564 BC-1382 Others , E1/E2/E3 Enzyme
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
T3549 Avadomide CC 122 Apoptosis , E1/E2/E3 Enzyme , Ligand for E3 Ligase
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
T3110 PRT4165 NSC600157,PRT 4165 BMI-1 , Others , E1/E2/E3 Enzyme
PRT4165 (NSC600157) is a potent PRC1-mediated H2A ubiquitylation inhibitor.
T16974 TAK-243 MLN7243 Apoptosis , E1/E2/E3 Enzyme , NF-κB
TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signaling as well as overall protein ubiquitination. TAK-243 exh...
T5555 Siremadlin NVP-HDM 201 E1/E2/E3 Enzyme
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T6254 Idasanutlin RG7388,Ro 5503781 Mdm2 , E1/E2/E3 Enzyme
Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
T6965 RG7112 RG-7112,RG 7112,RO5045337 Mdm2 , E1/E2/E3 Enzyme
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
T1493 BH3I-1 BHI1 BCL , E1/E2/E3 Enzyme
BH3I-1 (BHI1) is a Bcl-2 antagonist.
TQ0231 NVP-CGM097 CGM097 Mdm2 , E1/E2/E3 Enzyme
NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
TQ0127 Navtemadlin AMG232,CS-1300 Mdm2 , E1/E2/E3 Enzyme
Navtemadlin (AMG232) 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.
T6023 Nutlin-3a (-)-Nutlin-3,Nutlin-3a chiral,(−)-Nutlin-3 Apoptosis , E1/E2/E3 Enzyme , Autophagy
Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
T6611 NSC697923 2-[(4-methylphenyl)sulfonyl]-5-nitrofuran E1/E2/E3 Enzyme
NSC-697923 (2-[(4-methylphenyl)sulfonyl]-5-nitrofuran), a potent inhibitor of UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13), exhibits its role in inducing cell death in neuroblastoma (NB) cells through two distinct me...
T2243 Serdemetan JNJ-26854165 Apoptosis , Mdm2 , E1/E2/E3 Enzyme , p53
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T25465 GS143 GS-143,GS 143 IκB/IKK , E1/E2/E3 Enzyme , NF-κB
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 tran­scrip­tion of tar­get genes and does not inhibit protea...
T6585 SAR405838 MI773,MI 773,MI-77301,MI-773 Mdm2 , E1/E2/E3 Enzyme
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
T8929 BC1618 2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]- Mitophagy , Others , E1/E2/E3 Enzyme , AMPK
BC1618 (2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]-) is an orally active Fbxo48 inhibitor that stimulates Ampk-dependent signaling. It promotes mitochondrial fission, promotes autophagy and imp...
T6614 Nutlin-3b (+)-Nutlin-3 Mdm2 , E1/E2/E3 Enzyme
Nutlin-3b ((+)-Nutlin-3) 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 Nutlin-3a.
T28124 N106 N-106,N 106 E1/E2/E3 Enzyme
N106 is an activator of the SUMO-activating enzyme, E1 ligase, and triggers intrinsic sumoylation of SERCA2a. N106 can be used in studies about heart failure.

Compounds

Heclin
T24136
Synonym:
Target: E1/E2/E3 Enzyme
NAcM-OPT
T5374
Synonym:
Target: E1/E2/E3 Enzyme, NEDD8
SMIP004
T16901
Synonym:
Target: Apoptosis, Others, E1/E2/E3 Enzyme
RO8994
T3517
Synonym:
Target: Mdm2, E1/E2/E3 Enzyme, p53
Subasumstat
T8428
Synonym: TAK-981
Target: E1/E2/E3 Enzyme
ML-792
T16102
Synonym:
Target: E1/E2/E3 Enzyme
PYZD-4409
T16699
Synonym:
Target: Others, E1/E2/E3 Enzyme
COH000
T5199
Synonym:
Target: E1/E2/E3 Enzyme
Ubiquitination-IN-1
T13244
Synonym:
Target: Others
NSC232003
T12261
Synonym:
Target: E1/E2/E3 Enzyme
DKM 2-93
T7415
Synonym:
Target: E1/E2/E3 Enzyme
PYR-41
T6629
Synonym: PYR41,PYR 41
Target: Apoptosis, E1/E2/E3 Enzyme
Nutlin-3
T2158
Synonym: Nutlin3
Target: E1/E2/E3 Enzyme
2-D08
T7379
Synonym:
Target: E1/E2/E3 Enzyme, TAM Receptor
SJ-172550
T16888
Synonym:
Target: Mdm2, E1/E2/E3 Enzyme
WSB1 Degrader 1
T9236
Synonym:
Target: Others, E1/E2/E3 Enzyme
MX69
T3653
Synonym:
Target: Mdm2, E1/E2/E3 Enzyme, IAP
YH239-EE
T6149
Synonym:
Target: Apoptosis, E1/E2/E3 Enzyme
SZL P1-41
T3317
Synonym:
Target: Apoptosis, Others, E1/E2/E3 Enzyme
Skp2 Inhibitor C1
T4253
Synonym: SKPin C1
Target: Others, E1/E2/E3 Enzyme
MD-224
T11980
Synonym:
Target: Mdm2, E1/E2/E3 Enzyme, PROTACs
C25-140
T7889
Synonym:
Target: Others, TNF, E1/E2/E3 Enzyme, NF-κB
Mezigdomide
T10703
Synonym: CC-92480
Target: Apoptosis, E1/E2/E3 Enzyme, Molecular Glues
WS-383
T13349
Synonym:
Target: E1/E2/E3 Enzyme
SMER3
T23371
Synonym: SMER 3
Target: Others, Ligand for E3 Ligase
BC-1382
T8564
Synonym:
Target: Others, E1/E2/E3 Enzyme
Avadomide
T3549
Synonym: CC 122
Target: Apoptosis, E1/E2/E3 Enzyme, Ligand for E3 Ligase
PRT4165
T3110
Synonym: NSC600157,PRT 4165
Target: BMI-1, Others, E1/E2/E3 Enzyme
TAK-243
T16974
Synonym: MLN7243
Target: Apoptosis, E1/E2/E3 Enzyme, NF-κB
Siremadlin
T5555
Synonym: NVP-HDM 201
Target: E1/E2/E3 Enzyme
Idasanutlin
T6254
Synonym: RG7388,Ro 5503781
Target: Mdm2, E1/E2/E3 Enzyme
RG7112
T6965
Synonym: RG-7112,RG 7112,RO5045337
Target: Mdm2, E1/E2/E3 Enzyme
BH3I-1
T1493
Synonym: BHI1
Target: BCL, E1/E2/E3 Enzyme
NVP-CGM097
TQ0231
Synonym: CGM097
Target: Mdm2, E1/E2/E3 Enzyme
Navtemadlin
TQ0127
Synonym: AMG232,CS-1300
Target: Mdm2, E1/E2/E3 Enzyme
Nutlin-3a
T6023
Synonym: (-)-Nutlin-3,Nutlin-3a chiral,(−)-Nutlin-3
Target: Apoptosis, E1/E2/E3 Enzyme, Autophagy
NSC697923
T6611
Synonym: 2-[(4-methylphenyl)sulfonyl]-5-nitrofuran
Target: E1/E2/E3 Enzyme
Serdemetan
T2243
Synonym: JNJ-26854165
Target: Apoptosis, Mdm2, E1/E2/E3 Enzyme, p53
GS143
T25465
Synonym: GS-143,GS 143
Target: IκB/IKK, E1/E2/E3 Enzyme, NF-κB
SAR405838
T6585
Synonym: MI773,MI 773,MI-77301,MI-773
Target: Mdm2, E1/E2/E3 Enzyme
BC1618
T8929
Synonym: 2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]-
Target: Mitophagy, Others, E1/E2/E3 Enzyme, AMPK
Nutlin-3b
T6614
Synonym: (+)-Nutlin-3
Target: Mdm2, E1/E2/E3 Enzyme
N106
T28124
Synonym: N-106,N 106
Target: E1/E2/E3 Enzyme
Cat No. Product Name Synonyms Targets
T9352 Hydrocotarnine Others
hydrocotarnine is an inhibitor of Cbl.
T4S0181 Hinokiflavone MMP , BCL , E1/E2/E3 Enzyme
Hinokiflavone, a novel modulator of pre-mRNA splicing activity both in vitro and in cellulo, inhibits the assembly of the spliceosome, particularly blocking the formation of the B complex. Additionally, it acts as a SUMO...
T4036 Solasodine Solancarpidine,Purapuridine,Solasodin Apoptosis , Others , E1/E2/E3 Enzyme , Antifungal
Solasodine (Purapuridine)(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity against cervical cancer cell line (HeLa) and huma...
T2947 Indole-3-carbinol I3C,3-Indolemethanol,Indole-3-Methanol E1/E2/E3 Enzyme , NF-κB , Aryl Hydrocarbon Receptor , Endogenous Metabolite , p53
Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
T6S2123 Ginkgolic Acid Romanicardic acid,Ginkgolic acid I,Ginkgolic acid (15:1),Ginkgolic acid C15:1 Others , E1/E2/E3 Enzyme
Ginkgolic Acid (Romanicardic acid) C15:1 represses curli genes and prophage genes in EHEC.

Natural Products

hydrocotarnine
T9352
Synonym:
Target: Others
Hinokiflavone
T4S0181
Synonym:
Target: MMP, BCL, E1/E2/E3 Enzyme
Solasodine
T4036
Synonym: Solancarpidine,Purapuridine,Solasodin
Target: Apoptosis, Others, E1/E2/E3 Enzyme, Antifungal
Indole-3-carbinol
T2947
Synonym: I3C,3-Indolemethanol,Indole-3-Methanol
Target: E1/E2/E3 Enzyme, NF-κB, Aryl Hydrocarbon Receptor, Endogenous Metabolite, p53
Ginkgolic Acid
T6S2123
Synonym: Romanicardic acid,Ginkgolic acid I,Ginkgolic acid (15:1),Ginkgolic acid C15:1
Target: Others, E1/E2/E3 Enzyme

Recombinant Proteins

Species：
Human (15)
Expression System：
E. coli (11)
Baculovirus-Insect Cells (4)
Tag：
Tag Free (5)
His (4)
His,GST (2)
N-GST (2)
GST (1)
N-6His (1)
Cat No. Product Name Species Expression System
TMPY-02840 Ubiquitin Activating Enzyme E1/UBA1 Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
UBE1, also known as UBA1, belongs to the ubiquitin-activating E1 family. UBE1 gene complements an X-linked mouse temperature-sensitive defect in DNA synthesis, and thus may function in DNA repair. It is part of a gene cl...
TMPY-06748 UBA6 Protein, Human, Recombinant (GST) Human Baculovirus-Insect Cells
UBA6 (Ubiquitin Like Modifier Activating Enzyme 6) is a Protein Coding gene. The UBA6 gene, located on 4q13.2, is conserved in chimpanzee, Rhesus monkey, dog, cow, mouse, rat, chicken, zebrafish, and frog. Uba6 is a homo...
TMPJ-01324 UBA5 Protein, Human, Recombinant (His) Human E. coli
UBA5 is a member of the ubiquitin-activating E1 family and UBA5 subfamily. Ubiquitin and ubiquitin-like proteins are recognized as covalently conjugated to various cellular substrates by a three-step enzymatic pathway. T...
TMPY-03441 SAE1 Protein, Human, Recombinant Human Baculovirus-Insect Cells
SAE1 belongs to the ubiquitin-activating E1 family. It is a heterodimer that acts as a E1 ligase for SUMO1, SUMO2, SUMO3, and probably SUMO4. It functions as a UBLI E1 ligase mediating the ATP-dependent activation of UBL...
TMPY-03062 SAE1 Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
SAE1 belongs to the ubiquitin-activating E1 family. It is a heterodimer that acts as a E1 ligase for SUMO1, SUMO2, SUMO3, and probably SUMO4. It functions as a UBLI E1 ligase mediating the ATP-dependent activation of UBL...
TMPJ-00999 UBE2D1 Protein, Human, Recombinant (GST) Human E. coli
Ubiquitin-conjugating enzyme E2 D1（UBE2D1）belongs to the ubiquitin-conjugating enzyme family. Ubiquitination involves at least three classes of enzymes: ubiquitin-activating enzymes, or E1s, ubiquitin-conjugating enzymes...
TMPJ-01053 UBE2I Protein, Human, Recombinant (GST) Human E. coli
SUMO-Conjugating Enzyme UBC9 (UBC9) belongs to the ubiquitin-conjugating enzyme family. UBC9 is homologous to ubiquitin-conjugating enzymes (E2s). However, instead of conjugating ubiquitin, UBC9 conjugates a ubiquitin ho...
TMPY-02391 SUMO1 Protein, Human, Recombinant (His) Human E. coli
Small ubiquitin-like modifier protein (SUMO) modification is a highly dynamic process, catalyzed by SUMO-specific activating (E1), conjugating (E2) and ligating (E3) enzymes, and reversed by a family of SUMO-specific pro...
TMPY-02642 UBE2W Protein, Human, Recombinant (His) Human E. coli
Ubiquitin-conjugating enzymes, also known as UBE2W, E2 enzymes and more rarely as ubiquitin-carrier enzymes, perform the second step of protein ubiquitination. The modification of protein with ubiquitin is an important c...
TMPY-02609 UBE2M Protein, Human, Recombinant Human E. coli
UBE2M is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed ...
TMPY-02607 Ube2H Protein, Human, Recombinant Human E. coli
UBE2H is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed ...
TMPY-02608 UBC9/UBE2I Protein, Human, Recombinant Human E. coli
UBE2I is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed ...
TMPY-02606 UBE2G1 Protein, Human, Recombinant Human E. coli
UBE2G1 is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed...
TMPY-02605 UBE2F Protein, Human, Recombinant (His) Human E. coli
UBE2F is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed ...
TMPY-02604 UBE2D4 Protein, Human, Recombinant (His) Human E. coli
UBE2D4 is a member of the ubiquitin-conjugating E2 family whose members perform the second step in the ubiquitination reaction. Initially identified as the main process for protein degradation, ubiquitination is believed...
Cat No. Product Name
L8600 Ubiquitination Compound Library

214 compounds
A unique collection of 214 ubiquitination related small chemicals can be used for high throughput and high content screening；

Libraries

Ubiquitination Compound Library
L8600
Compounds: 214
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