Chemical Structure : HA-218-6-31-80
CAS No.:
HA-218-6-31-80
Catalog No.: PC-27546Not For Human Use, Lab Use Only.
HA-218-6-31-80 is a novel NEDD8-activating enzyme (NAE) inhibitor, directly binds NAE and suppresses its catalytic activity, blocks the formation of E2-NEDD8 thioesters, and reduces the neddylation of CUL1 and CUL5 in purified protein systems.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HA-218-6-31-80 is a novel NEDD8-activating enzyme (NAE) inhibitor, directly binds NAE and suppresses its catalytic activity, blocks the formation of E2-NEDD8 thioesters, and reduces the neddylation of CUL1 and CUL5 in purified protein systems.
HA-218-6-31-80 potently suppresses neddylation of multiple CUL family members, leading to the accumulation of CRL substrates including p27 and NOXA, in human lung cancer cells.
HA-218-6-31-80 riggers G1-phase arrest and NOXA-dependent apoptosis, inhibiting lung cancer cell proliferation and survival.
HA-218-6-31-80 significantly suppresses tumor growth without obvious systemic toxicity in A549 xenograft models.
Physicochemical Properties
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M.Wt
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528.77
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Formula
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C32H40N2O3Si
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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7-(2-hydroxy-3-methoxybenzyl)-N-(3'-(trimethylsilyl)-[1,1'-biphenyl]-3-yl)-7-azaspiro[3.5]nonane-2-carboxamide
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References
1. Chen Q, et al. RSC Med Chem. 2026 Jul 17. doi: 10.1039/d6md00393a.
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