Chemical Structure : 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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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.
| 分子量 | 528.77 | |
| 分子式 | C32H40N2O3Si | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Chen Q, et al. RSC Med Chem. 2026 Jul 17. doi: 10.1039/d6md00393a.
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