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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) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.
  • $48
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Milademetan
T120401398568-47-2In house
Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.
  • $89
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Nutlin-3a
T6023675576-98-4
Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.
  • $45
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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.
  • $35
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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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Subasumstat
T84281858276-04-6
Subasumstat (TAK-981), a selective inhibitor of the SUMOylation enzymatic cascade, has potential immune-activating and antineoplastic activities.
  • $76
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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), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis.
  • $41
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ML-792
T161021644342-14-2
ML-792 is a specific small ubiquitin-like modifier activating enzyme (SUMO) inhibitor. ML-792 selectively inhibits SAE SUMO1 and SAE SUMO2 with IC50 of 3 and 11 nM.
  • $84
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DT204
T71830428497-71-6In house
DT204 is an SCFSkp2 inhibitor that reduces the binding of Skp2 to Cullin-1 and Commd1. It can be used to study multiple myeloma.
  • $293
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Cbl-b-IN-3
T637902573775-59-2In house
Cbl-b-IN-3 is a potent inhibitor of casitas b lineage lymphoma proto-oncogene-b (Cbl-b) (ic50 < 1 nM).
  • $64
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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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Brigimadlin
T699232095116-40-6
Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.
  • $162
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C25-140
T78891358099-18-9
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
  • $68
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Alrizomadlin
T143031818393-16-6
Alrizomadlin is an orally active MDM2 inhibitor. APG-115 shows significant dose-dependent inhibitory effects on TP53wt AML cell lines. The IC50 values ​​are 26.8 nM for MOLM-13 cells and 165.9 nM for MV-4-11 cells. , OCI-AML-3 cells 315.6 nM. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell cycle arrest and apoptosis in a p53-dependent manner.
  • $48
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Ginkgolic Acid
T6S212322910-60-7
Ginkgolic Acid (Romanicardic acid) C15:1 represses curli genes and prophage genes in EHEC.
  • $33
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Nutlin-3
T2158548472-68-0
Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity.
  • $31
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RG7112
T6965939981-39-2
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
  • $41
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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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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).
  • $198
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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.
  • $30
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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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Mezigdomide
T107032259648-80-9In house
Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]
  • $118
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HOIPIN-8 sodium
T628262519537-70-1
HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.
  • $64
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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.
  • $38
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