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HDAC3 inhibitor PT3

Chemical Structure : HDAC3 inhibitor PT3

CAS No.: 2710273-81-5

HDAC3 inhibitor PT3 (ESI1, Epigenetic-silencing-inhibitor)

货号: PC-72343Not For Human Use, Lab Use Only.

HDAC3 inhibitor PT3 (ESI1) is a novel potent, selective, BBB-permeable HDAC3 inhibitor with IC50 of 250 nM, promotes CNS myelin production and regeneration.

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纯度 & COA & 质检文件 纯度: 99.5% (HPLC) Select Batch:

生物&药学活性

HDAC3 inhibitor PT3 (ESI1) is a novel potent, selective, BBB-permeable HDAC3 inhibitor with IC50 of 250 nM, promotes CNS myelin production and regeneration.
PT3 exhibited higher selectivity for HDAC3 over HDAC1, HDAC6, and HDAC8 compared to the reference compound CI994.
PT3 upregulated H3K9 acetylation, CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43 and MMP9 expression in mouse neuronal (N2A) cells.
PT3 significantly improved the discrimination index in C57/BL6 mice in the novel object recognition (NOR) model, significant increased in H3K9 acetylation in hippocampus.
PT3 upregulated CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43, PSD 95 and MMP9 expression in mice treated with PT3.
ESI1 triggered nuclear condensate formation of master lipid-metabolic regulators SREBP1/2, concentrating transcriptional co-activators to drive lipid/cholesterol biosynthesis.
ESI1 enhances (re)myelination in aged mice while reversing cognitive decline

物理化学性质&存储条件

分子量 319.368
分子式 C18H17N5O
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

N-(2-aminophenyl)-5-(benzylamino)pyrazine-2-carboxamide

参考文献

1. Sravani Pulya, et al. ACS Chem Neurosci. 2021 Mar 3;12(5):883-892.
2. Liu X, et al. Cell. 2024 Apr 25:S0092-8674(24)00400-8.

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