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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-PB118
PB118

Chemical Structure : PB118

CAS No.:

PB118 (HDAC6i PB118)

货号: PC-21394Not For Human Use, Lab Use Only.

PB118 is a potent, selective HDAC6 inhibitor with IC50 of 5.6 nM, shows >1000 times selectively towards HDAC1, reduces alzheimer's disease neuropathology.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PB118 is a potent, selective HDAC6 inhibitor with IC50 of 5.6 nM, shows >1000 times selectively towards HDAC1, reduces alzheimer's disease neuropathology.
PB118 displays >100-fold selectivity compared to other histone deacetylases (HDACs).
PB118 significantly impacts the aggregation-prone Aβ42 protein and increased its phagocytosis, a process for clearing cell debris and protein aggregates in microglia BV2 cell.
PB118 significantly increases the acetylated α-tubulin levels in BV2 cell, which is a measure of stable microtubule, by inhibiting the activity of HDAC6.
PB118 reduces the IL-6, IL-12p-70, and KC/GRO (CXCL1) cytokines and chemokines which are responsible for neuroinflammatory changes in Alzheimer's disease (AD).
PB118 significantly reduces p-tau levels and Aβ42 generation on 3D-AD human neural culture model.

物理化学性质&存储条件

分子量 314.36
分子式 C18H19FN2O2
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

3-fluoro-N-hydroxy-4-((2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)methyl)benzamide

参考文献

1. Mondal P, et al. Adv Sci (Weinh). 2023 Nov 21:e2304545.

2. Ping Bai, et al. Acta Pharm Sin B. 2022 Oct;12(10):3891-3904.

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