E1 Activating

E1 Activating製品

All (10)
E1 Activating阻害剤 (10)
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
S7109	Pevonedistat (MLN4924)	MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.	Cell Rep Med, 2025, 6(2):101927 Biomolecules, 2025, 15(1)76 BMC Biol, 2025, 23(1):51
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.	Int Immunopharmacol, 2025, 145:113742 J Virol, 2025, e0191224. J Gen Virol, 2025, 106(1)002063
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.	Redox Biol, 2025, 81:103522 Bioact Mater, 2024, 32:277-291 Int J Mol Sci, 2024, 25(5)2768
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.
E1953^New	Pevonedistat hydrochloride	Pevonedistat 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952^New	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 leukemia cells and can be used as a research for developing treatments for hematologic malignancies.
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 Neurooncol Adv, 2024, 6(1):vdae104
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.	Cell Rep Med, 2025, 6(2):101927 Biomolecules, 2025, 15(1)76 BMC Biol, 2025, 23(1):51
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.	Int Immunopharmacol, 2025, 145:113742 J Virol, 2025, e0191224. J Gen Virol, 2025, 106(1)002063
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.	Redox Biol, 2025, 81:103522 Bioact Mater, 2024, 32:277-291 Int J Mol Sci, 2024, 25(5)2768
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.
E1953^New	Pevonedistat hydrochloride	Pevonedistat 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952^New	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 leukemia cells and can be used as a research for developing treatments for hematologic malignancies.
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 Neurooncol Adv, 2024, 6(1):vdae104
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).
E1953^New	Pevonedistat hydrochloride	Pevonedistat 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952^New	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 leukemia cells and can be used as a research for developing treatments for hematologic malignancies.

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E1 Activatingシグナル伝達経路