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.
Targets for E1/E2/E3 Enzyme
Products for E1/E2/E3 Enzyme
- Cat.No. Product Name Information
- GC10408 2-D08 Sumoylation inhibitor
- GC33356 AM-8735 AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
- GC15828 AMG232 AMG232 (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG232 binds to MDM2 with a Kd of 0.045 nM.
- GC35367 APG-115 APG-115 (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
- GC68150 BC-1382
- GC62135 BC1618 BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation).
- GC18136 BH3I-1 Bcl-2 or Bcl-XL inhibitor
- GC35511 BI-0252 BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
- GC65305 BI8622 BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
- GC65148 BI8626 BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM.
- GC34513 C25-140 C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13.
- GC62568 Cbl-b-IN-1 Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM.
- GC39169 CC-92480 CC-92480 (CC-92480), a cereblon E3 ubiquitin ligase modulating drug (CELMoD), acts as a molecular glue. CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.
- GC35625 CC0651 CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
- GC19088 CC122 CC122 (CC 122) is an orally active cereblon modulator.
- GC33039 COH000 COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
- GC32911 CTX1 CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
- GC65576 DI-1859 DI-1859 is a potent, selective and covalent inhibitor of DCN1.
- GC62721 DI-591 DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12?nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members.
- GC32814 DKM 2-93 DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
- GC10134 Ginkgolic Acid C15:1 Ginkgolic Acid C15:1 is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
-
GC43786
GS-143
GS-143 is an inhibitor of IκBα ubiquitylation.
- GC63002 HB007 HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
- GC38488 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 spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
- GC63004 HOIPIN-8 HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM.
- GC16368 Indole-3-carbinol anticarcinogenic drug
- GC12117 JNJ-26854165 (Serdemetan) An antagonist of MDM2 action
- GC63363 M435-1279 M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
- GC62716 MD-222 MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
- GC38812 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
- GC36605 MI-1061 MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
- GC62598 MI-1061 TFA MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
- GC16296 MI-773 MDM2 inhibitor
- GC11547 MI-773 (SAR405838) MI-773 (SAR405838) (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. MI-773 (SAR405838) binds to MDM2 with a Ki of 0.88 nM. MI-773 (SAR405838) induces apoptosis and has potent antitumor activity.
- GC32881 Milademetan (DS-3032) Milademetan (DS-3032) (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
- GC62621 Milademetan tosylate hydrate Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
- GC36631 ML-792 ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50 values of 32 μM and >100 μM, respectively).
- GC19257 MX69 MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
- GC64989 NAcM-OPT NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.
- GC32721 NSC232003 NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
- GC16051 Nutlin-3 A racemic mixture of (?)-nutlin-3 and (+)-nutlin-3
- GC10470 Nutlin-3a chiral An inhibitor of the p53-Mdm2 interaction
- GC12508 Nutlin-3b MDM2/p53 inhibitor
- GC12647 NVP-CGM097 potent and selective MDM2 inhibitor
- GC36785 NVP-CGM097 sulfate NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
- GC19268 NVP-HDM201 NVP-HDM201 (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
- GC36835 p53 and MDM2 proteins-interaction-inhibitor chiral p53 and MDM2 proteins-interaction-inhibitor chiral (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
- GC36836 p53 and MDM2 proteins-interaction-inhibitor dihydrochloride p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
- GC36837 p53 and MDM2 proteins-interaction-inhibitor racemic p53 and MDM2 proteins-interaction-inhibitor racemic (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
- GC37010 PROTAC MDM2 Degrader-1 PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37011 PROTAC MDM2 Degrader-2 PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37012 PROTAC MDM2 Degrader-3 PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37013 PROTAC MDM2 Degrader-4 PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC10940 PRT 4165 Bmi1/Ring1A-mediated ubiquitination inhibitor
-
GC15771
PYR-41
inhibitor of Ubiquitin-Activating Enzyme (E1)
- GC17801 PYZD-4409 E1 enzyme inhibitor
- GC65605 RB-3 RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.
- GC13019 RG7112 An inhibitor of the MDM2-p53 interaction
- GC11594 RG7388 An inhibitor of the MDM2-p53 interaction
- GC37549 RO-5963 RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.
- GC19312 RO8994 RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).
-
GC69842
Rugonersen
Rugonersen (RG6091; RO7248824) is an antisense oligonucleotide (ASO) modified with locked nucleic acid (LNA), which reduces the silencing of ubiquitin protein ligase E3A (UBE3A). Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A. Rugonersen has been used in research on AS.
-
GC69866
SCFSkp2-IN-2
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis in NSCLC cells and exhibits anti-tumor activity.
- GC65469 SENP1-IN-1 SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
- GC13590 SJ 172550 A small molecule inhibitor of MDMX
-
GC69911
Skp2 inhibitor 1
Skp2 inhibitor 1 (compound 14i) is a Skp2 inhibitor that disrupts the Skp2-Cks1 interaction, with an IC50 of 2.8 μM. Skp2 inhibitor 1 also exhibits anti-cancer activity.
- GC37648 Skp2 Inhibitor C1 An inhibitor of Skp2-mediated p27 degradation
- GC16055 SMIP004
- GC16371 Solasodine An alkaloid with diverse biological activities
- GC64972 Subasumstat Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
- GC11869 SZL P1-41 Skp2 inhibitor
- GC32737 TAK-243 (MLN7243) TAK-243 (MLN7243) (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
- GC65881 Teslexivir hydrochloride Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.
- GC18561 TZ9 TZ9 is a cell-permeable triazine compound that inhibits the human E2 ubiquitin-conjugating enzyme Rad6B.
-
GC70082
UBA5-IN-1
UBA5-IN-1 (compound 8.5) is a selective inhibitor of UBA5 with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits the proliferation of Sk-Luci6 cancer cells that overexpress UBA5.
- GC33885 UbcH5c-IN-1 UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85.
- GC64033 Ubiquitination-IN-1 Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
- GC64975 WS-383 WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
- GC62343 WSB1 Degrader 1 WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.
- GC11445 YH239-EE p53-MDM2 antagonist, potent