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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.

  • Pevonedistat
    T6332905579-51-3
    Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM). Pevonedistat can be used for the treatment of myelodysplastic syndromes (MDS) and also has antitumor activity.
    • $48
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  • ML-792
    T161021644342-14-2
    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 inhibitor of SAE/SUMO1 and SAE/SUMO2 in
    • $84
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  • Mezigdomide
    T107032259648-80-9In house
    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.
    • $118
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  • Cbl-b-IN-3
    T637902573775-59-2In house
    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 the setting of T lymphocyte activation thresholds. Cpl-b negatively regulates p85 in an independent proteolytic manner, and participates in the recruitment of p85 to CD28 and T cell antigen receptor ζ through its E3 ubiquitin ligase activity. Inhibition of PI3K inhibits the enhancement of Cblb-/ -T cell activation.
    • $383
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  • Navtemadlin
    TQ01271352066-68-2
    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.
    • $67
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  • Indole-3-carbinol
    T2947700-06-1
    Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
    • $29
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  • Ginkgolic Acid
    T6S212322910-60-7
    Ginkgolic Acid (Romanicardic acid) C15:1 represses curli genes and prophage genes in EHEC.
    • $100
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  • ZM223
    T134122031177-48-5
    ZM223 is an inhibitor of NEDD8 activating enzyme (NAE).
    • $117
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  • NSC697923
    T6611343351-67-7In house
    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 mechanisms. In p53 wild-type NB cells, NSC-697923 promotes the nuclear importation of p53, thereby triggering cell death. Meanwhile, in p53 mutant NB cells, NSC-697923 activates the JNK-mediated apoptotic pathway, leading to cell death. Additionally, NSC-697923 inhibits DNA damage and NF-κB signaling, further contributing to its antitumor activity.
    • $39
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  • SAR405838
    T65851303607-60-4In house
    MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
    • $45
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  • Nutlin-3
    T2158548472-68-0
    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.
    • $54
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  • PRT4165
    T311031083-55-3
    PRT4165 (NSC600157) is a potent PRC1-mediated H2A ubiquitylation inhibitor.
    • $38
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  • C25-140
    T78891358099-18-9
    C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
    • $68
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  • Idasanutlin
    T62541229705-06-9
    Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
    • $34
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  • Serdemetan
    T2243881202-45-5
    Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
    • $39
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  • 2-D08
    T7379144707-18-6
    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.
    • $52
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  • NAE-IN-M22
    T8816864420-54-2
    NAE-IN-M22 (NEDD8 inhibitor M22) is a selective, potent and reversible inhibitor of NEDD8 activating enzyme (NAE). NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
    • $93
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  • Hinokiflavone
    T4S018119202-36-9
    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 protease inhibitor by impeding the activity of sentrin-specific protease 1 (SENP1). Hinokiflavone also demonstrates significant cytotoxicity, including the inhibition of MMP-9.
    • $39
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  • TAK-243
    T169741450833-55-2
    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 exhibits antitumor activity and promotes apoptosis.
    • $41
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  • COH000
    T51991534358-79-6
    COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
    • $228
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  • PYR-41
    T6629418805-02-4
    PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
    • $33
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  • Nutlin-3b
    T6614675576-97-3
    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.
    • $35
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  • UC-764864
    T79133278806-03-4
    UC-764864 is a selective UBE2N inhibitor that blocks E1-UBE2N thioester transfer, inhibits innate immune signaling and induces cytotoxic effects in MDS/AML cell lines and primary cells. In addition, UC-764864 reduces the ubiquitination status of UBE2N and can be used to study leukemia.
    • $107
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  • Cbl-b-IN-6
    T798932815221-33-9
    Cbl-b-IN-6 (Compound 246) is an inhibitor of both casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, exhibiting inhibitory half-maximal inhibitory concentrations (IC50s) of 6.7 nM for Cbl-b and 5.2 nM for c-Cbl, respectively [1].
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  • Cbl-b-IN-9
    T798962815223-41-5
    Cbl-b-IN-9 (Compound 300) is an inhibitor targeting casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, exhibiting potent inhibitory activity with half-maximal inhibitory concentrations (IC50s) of 5.6 nM and 4.7 nM, respectively [1].
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  • Cbl-b-IN-12
    T798992851871-29-7
    Cbl-b-IN-12 (Example 10) is an inhibitor of casitas B-lineage lymphoma-b (CBL-B), demonstrating a half-maximal inhibitory concentration (IC50) of less than 100 nM [1].
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  • TRAF6 peptide TFA
    T78221
    TRAF6 peptide TFA, a specific inhibitor of the TRAF6-p62 interaction, significantly inhibits NGF-dependent ubiquitination of TrkA. This peptide demonstrates promising research applications in various neurological disorders, including Alzheimer's disease (AD), Parkinson's, ALS, head trauma, epilepsy, and stroke [1].
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  • Skp2 inhibitor 2
    T781942760612-77-7
    Skp2 inhibitor 2 (14f) impedes the F-box protein S-phase kinase-associated protein 2 (Skp2), demonstrating an IC50 of 10.2 μM against Skp2-Cks1. This compound targets Skp2, a component of cullin-RING ligases that recruits and ubiquitinates substrates, playing roles in both proteolytic and non-proteolytic processes [1].
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  • SJ-172550
    T16888431979-47-4
    SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
    • $37
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  • SMIP004
    T16901143360-00-3
    SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.
    • $82
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  • TAS4464
    T13090L1848959-10-3
    TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
      7-10 days
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    • Subasumstat
      T84281858276-04-6
      Subasumstat (TAK-981) is a selective the SUMOylation enzymatic cascade inhibitor, has potential immune-activating and antineoplastic activities.
      • $76
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    • Heclin
      T24136890605-54-6
      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.
      • $39
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    • Cbl-b-IN-11
      T798982815225-15-9
      Cbl-b-IN-11 (Compound 466) is an inhibitor of both casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, exhibiting half-maximal inhibitory concentrations (IC50s) of 6.4 nM and 6.1 nM, respectively [1].
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    • Smurf1-IN-1
      T787211824708-03-3
      Smurf1-IN-1, a selective E3 ubiquitin protein ligase 1 (SMURF1) inhibitor, exhibits oral activity with an IC50 of 92 nM and demonstrates considerable efficacy in a rat model of pulmonary hypertension [1].
      • $1,520
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    • WSB1 Degrader 1
      T92362306039-66-5
      WSB1 Degrader 1 is a potent, orally active degrader of WD repeat and SOCS box-containing 1, exhibiting anti-cancer metastatic effects.
      • $97
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    • GS143
      T25465916232-21-8
      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 proteasome activity. GS143 has anti-asthm
      • $38
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    • N106
      T28124862974-25-2
      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.
      • $43
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    • Skp2 Inhibitor C1
      T4253432001-69-9
      Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
      • $36
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    • NSC232003
      T122611905453-18-0
      NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
      • $90
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    • Cbl-b-IN-13
      T799002368841-85-2
      Cbl-b-IN-13 (Example 520) is a potent Cbl-b inhibitor exhibiting an IC50 of less than 100 nM and is capable of activating T-cells [1].
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    • BC-1382
      T85641013753-99-5
      BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).
      • $91
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    • Nutlin-3a
      T6023675576-98-4
      Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
      • $45
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    • Siremadlin
      T55551448867-41-1
      Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
      • $61
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    • Cbl-b-IN-7
      T798942815221-35-1
      Cbl-b-IN-7 (Compound 248) is an inhibitor of casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, exhibiting inhibitory half-maximal inhibitory concentrations (IC50s) of 6.7 nM and 5.2 nM, respectively [1].
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    • Cbl-b-IN-8
      T798952815223-33-5
      Cbl-b-IN-8 (Compound 293) is an inhibitor of both casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, exhibiting half maximal inhibitory concentrations (IC50s) of 5.5 nM and 7.8 nM, respectively [1].
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    • NAcM-OPT
      T53742089293-61-6
      NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
      • $43
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    • MD-224
      T119802136247-12-4
      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.
      • $64
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    • TAS4464 hydrochloride
      T130901848959-11-4
      TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).
      • $61
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    • WS-383
      T133492247544-02-9
      WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).
      • $38
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