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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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.
S5841 DKM 2-93 DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5).
S7109 Pevonedistat (MLN4924) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.
Nat Cell Biol, 2022, 24(3):384-399
Blood Cancer J, 2022, 12(3):39
Cell Rep, 2022, 39(2):110690
S7129 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. PYR-41 induce apoptosis.
Sci Adv, 2021, 7(21)eabg4168
J Clin Invest, 2021, 146893
Biomaterials, 2021, 271:120720
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 NFκB pathway activation and promotes apoptosis.
Cell Rep, 2022, 38(12):110538
Free Radic Biol Med, 2022, 183:89-103
Arch Toxicol, 2022, 10.1007/s00204-021-03195-w
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.
Cell Rep, 2022, 38(12):110538
Cancer Sci, 2022, 113(2):622-633
Front Pharmacol, 2021, 12:731980
S8849 TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition.
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.
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.
S5841 DKM 2-93 DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5).
S7109 Pevonedistat (MLN4924) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.
Nat Cell Biol, 2022, 24(3):384-399
Blood Cancer J, 2022, 12(3):39
Cell Rep, 2022, 39(2):110690
S7129 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. PYR-41 induce apoptosis.
Sci Adv, 2021, 7(21)eabg4168
J Clin Invest, 2021, 146893
Biomaterials, 2021, 271:120720
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 NFκB pathway activation and promotes apoptosis.
Cell Rep, 2022, 38(12):110538
Free Radic Biol Med, 2022, 183:89-103
Arch Toxicol, 2022, 10.1007/s00204-021-03195-w
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.
Cell Rep, 2022, 38(12):110538
Cancer Sci, 2022, 113(2):622-633
Front Pharmacol, 2021, 12:731980
S8849 TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition.
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