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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-NEDD8-activating Enzyme (NAE)-HA-218-6-31-80
HA-218-6-31-80

Chemical Structure : HA-218-6-31-80

CAS No.:

HA-218-6-31-80

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 528.77
分子式 C32H40N2O3Si
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-(2-hydroxy-3-methoxybenzyl)-N-(3'-(trimethylsilyl)-[1,1'-biphenyl]-3-yl)-7-azaspiro[3.5]nonane-2-carboxamide

参考文献

1. Chen Q, et al. RSC Med Chem. 2026 Jul 17. doi: 10.1039/d6md00393a.

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