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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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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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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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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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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).
  • $383
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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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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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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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Ginkgolic Acid
T6S212322910-60-7
Ginkgolic Acid (Romanicardic acid) C15:1 represses curli genes and prophage genes in EHEC.
  • $33
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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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C25-140
T78891358099-18-9
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
  • $68
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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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NSC232003
T122611905453-18-0
NSC232003 is a highly potent and cell-permeable inhibitor of [UHRF1].
  • $90
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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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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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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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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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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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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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Siremadlin
T55551448867-41-1
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
  • $55
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ZM223
T134122031177-48-5
ZM223 is an inhibitor of NEDD8 activating enzyme (NAE).
  • $117
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BC-1382
T85641013753-99-5
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specifically disrupts the HECTD2 PIAS1 interaction(IC50 of 5 nM).
  • $81
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BI8626
T145691875036-75-1
BI8626 is a ubiquitin ligase HUWE1 inhibitor with protective effects against spontaneous desiccation syndrome in NOD ShiLtj mice.BI8626 inhibits intracellular cholesterol and decreases the expression of phosphorylated ZAP-70, CD25, and other activation markers, and inhibits the proliferation of CD4 T-cells.
  • $84
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Avadomide
T35491015474-32-4
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
  • $40
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