E1 Activating

E1 Activating製品

All (8)
E1 Activating阻害剤 (8)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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 Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01257-y Nat Commun, 2024, 15(1):4584
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 Commun, 2024, 15(1):2485
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 highly potent and selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM.	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 Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01257-y Nat Commun, 2024, 15(1):4584
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 Commun, 2024, 15(1):2485
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 highly potent and selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM.	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).

E1 Activating阻害剤の選択性比較

E1 Activatingシグナル伝達経路

E1 Activatingシグナル伝達経路

Tags: E1 Activating inhibitor|E1 Activating agonist|E1 Activating activator|E1 Activating inducer|E1 Activating antagonist|E1 Activating signaling pathway|E1 Activating assay kit