E1 Activating

E1 Activating製品

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  • E1 Activating阻害剤 (10)
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S7109 Pevonedistat (MLN4924) 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
Pevonedistat-S710901W0420190221.gif
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.
Mol Cell, 2025, 85(18):3505-3523.e17
Leukemia, 2025, 39(8):1997-2009.
Mol Syst Biol, 2025, 10.1038/s44320-025-00109-1
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.
Nat Commun, 2025, 16(1):3756
Redox Biol, 2025, 81:103522
EMBO Rep, 2025, 10.1038/s44319-025-00444-2
PYR-41-S712901W0620161128.gif
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
F0109 Ubiquitin Antibody [J9C13] Ubiquitin Rabbit mAb recognizes endogenous levels of total Ubiquitin protein.
Am J Cancer Res, 2025, 15(8):3449-3459
F0320New Atg7 Antibody [K21F3] Atg7 Rabbit mAb recognizes endogenous levels of total Atg7 protein.
F1956 NAE1/APPBP1 Antibody [N23N11]
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
E1953New 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952New 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).
Cell Rep, 2025, 44(10):116433
S7109 Pevonedistat (MLN4924) 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
Pevonedistat-S710901W0420190221.gif
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.
Mol Cell, 2025, 85(18):3505-3523.e17
Leukemia, 2025, 39(8):1997-2009.
Mol Syst Biol, 2025, 10.1038/s44320-025-00109-1
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.
Nat Commun, 2025, 16(1):3756
Redox Biol, 2025, 81:103522
EMBO Rep, 2025, 10.1038/s44319-025-00444-2
PYR-41-S712901W0620161128.gif
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
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
E1953New 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952New 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).
Cell Rep, 2025, 44(10):116433
F0320New Atg7 Antibody [K21F3] Atg7 Rabbit mAb recognizes endogenous levels of total Atg7 protein.
E1953New 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 tumor cells through the deregulation of S-phase DNA synthesis.
E7952New 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.

E1 Activatingシグナル伝達経路