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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-EKZ-438
EKZ-438

Chemical Structure : EKZ-438

CAS No.:

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EKZ-438 (EKZ438)

货号: PC-25868Not For Human Use, Lab Use Only.

EKZ-438 is a potent, selective, CNS-penetrant and orally bioavailable HDAC6 inhibitor with IC50 of 12 nM, >8,500-fold selectivity for HDAC6 versus all other HDAC6 paralogs.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

EKZ-438 is a potent, selective, CNS-penetrant and orally bioavailable HDAC6 inhibitor with IC50 of 12 nM, >8,500-fold selectivity for HDAC6 versus all other HDAC6 paralogs.
EKZ-438 selectively inhibits catalytic domain 2 of HDAC6 to increase α-tubulin acetylation.
EKZ-438 selectively inhibits HDAC6 and ameliorates excitotoxicity in a cellular model of ALS.
EKZ-438 improves axonal transport and motor function in a mouse model of familial ALS.
EKZ-438 reduces accumulation of cytoplasmically mislocalized TDP-43 in an autophagy-dependent manner.
EKZ-438 improves TDP-43 proteostasis and reduces neuroinflammation in a mouse model of ALS and FTD.

物理化学性质&存储条件

分子量
分子式
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

参考文献

1. James RE, et al. Brain. 2025 Oct 8:awaf380.

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