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E1 Activating inhibitors

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DUB E2 conjugating E3 Ligase p97 SUMO
Cat.No. Product Name Information Product Use Citations Product Validations
S7109 MLN4924 (Pevonedistat) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.
Nature, 2025, 642(8068):785-795
Nat Commun, 2025, 16(1):2526
Nat Commun, 2025, 16(1):3756
Verified customer review of MLN4924 (Pevonedistat)
S8341 TAK-243 (MLN7243) TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NF-κB pathway activation and promotes apoptosis.
Mol Cell, 2025, 85(18):3505-3523.e17
Leukemia, 2025, 39(8):1997-2009.
J Nanobiotechnology, 2025, 23(1):717
S7129 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. This compound induces apoptosis.
Nat Commun, 2025, 16(1):3756
Redox Biol, 2025, 81:103522
EMBO Rep, 2025, 10.1038/s44319-025-00444-2
Verified customer review of PYR-41
S8697 ML792 ML-792 is a potent and selective inhibitor of SUMO (small ubiquitin-like modifier)-activating enzyme (SAE). ML-792 inhibits SAE/SUMO1 and SAE/SUMO2 in ATP–inorganic pyrophosphate (PPi) exchange assays with IC50 of 3 nM and 11 nM, respectively.
Mol Cell, 2025, 85(5):877-893.e9
Nat Cell Biol, 2024, 10.1038/s41556-024-01394-y
Genes Dev, 2024, 38(13-14):614-630
S8849 TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. This compound exhibits superior antitumor activity with prolonged target inhibition.
Nat Commun, 2024, 15(1):603
Neurooncol Adv, 2024, 6(1):vdae104
S0309 COH000 COH000 is an allosteric, covalent and irreversible ubiquitin-like 1-activating enzyme (SUMO-activating enzyme / E1) inhibitor with IC50 of 0.2 μM for SUMOylation in vitro.
iScience, 2025, 28(6):112555
S5841 DKM 2-93 DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5).
Cell Rep, 2025, 44(10):116433
E1953 Pevonedistat hydrochloride Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective inhibitor of NEDD8-activating enzyme (NAE) with an IC50 of 4.7 nM. It disrupts cullin-RING ligase-mediated protein degradation, leading to apoptotic cell death in human tumour cells through the deregulation of S-phase DNA synthesis.
E7952 PYZD-4409 PYZD-4409 is a potent and specific small molecule inhibitor of the ubiquitin-activating enzyme UBA1 (E1) with an IC50 of 20 μM. It induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukaemia cells and can be used as a research for developing treatments for haematologic malignancies.
S3400 NEDD8 inhibitor M22 NEDD8 inhibitor M22 (NAE-IN-M22) is a novel selective NEDD8 activating enzyme (NAE) inhibitor with GI50 of 5.5 μM in A549 cells.