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Catalog No. Product Name Information Product Use Citations Product Validations
S7109 Pevonedistat (MLN4924) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):242
Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01257-y
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, 2024, 187(21):6055-6070.e22
Cell, 2024, 187(21):5967-5980.e17
Nat Cell Biol, 2024, 26(11):1943-1957
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.
Bioact Mater, 2024, 32:277-291
Int J Mol Sci, 2024, 25(5)2768
Viruses, 2024, 16(2)290
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.
Nat Cell Biol, 2024, 10.1038/s41556-024-01394-y
bioRxiv, 2024, 2024.02.29.582813
Nat Struct Mol Biol, 2023, 10.1038/s41594-023-01045-0
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.
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.
Nat Commun, 2024, 15(1):603
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.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):242
Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01257-y
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, 2024, 187(21):6055-6070.e22
Cell, 2024, 187(21):5967-5980.e17
Nat Cell Biol, 2024, 26(11):1943-1957
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.
Bioact Mater, 2024, 32:277-291
Int J Mol Sci, 2024, 25(5)2768
Viruses, 2024, 16(2)290
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.
Nat Cell Biol, 2024, 10.1038/s41556-024-01394-y
bioRxiv, 2024, 2024.02.29.582813
Nat Struct Mol Biol, 2023, 10.1038/s41594-023-01045-0
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.
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.
Nat Commun, 2024, 15(1):603
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).

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