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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-FLAV-27
FLAV-27

Chemical Structure : FLAV-27

CAS No.:

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FLAV-27 (FLAV27)

货号: PC-25914Not For Human Use, Lab Use Only.

FLAV-27 is a potent, selective, SAM-competitive, brain-penetrant inhibitor of histone methyltransferase G9a with IC50 of 0.6 nM, with excellent selectivity over GLP (3.2% inhibition at 1 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FLAV-27 is a potent, selective, SAM-competitive, brain-penetrant inhibitor of histone methyltransferase G9a with IC50 of 0.6 nM, with excellent selectivity over GLP (3.2% inhibition at 1 uM).
FLAV-27 demonstrates high selectivity for G9a, showing less than 15% inhibition at 1 μM across a panel of 32 HMTs, including H3K9 (SUV39H1, SUV39H2, and SUV420H1), H3K27 (enhancer of zeste homolog 2 (EZH2)), H3K4 (SET domain containing 7 (SETD7) and mixed lineage leukemia (MLL)), H3K79 (disruptor of telomeric silencing 1-like (DOT1L)), and H4K20 (SETD8), as well as various protein arginine methyltransferases (PRMTs).
FLAV-27 exhibits robust central nervous system bioavailability.
FLAV-27 reduces amyloid beta (Aβ) and p-tau aggregation and restores neuritic complexity in vitro.
FLAV-27 improves mobility, lifespan, and mitochondrial respiration in Caenorhabditis elegans.
FLAV-27 rescues memory performance, social behavior, and synaptic structure in mouse models of both late-onset AD (SAMP8) and early-onset AD (5xFAD).

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. Bellver-Sanchis A, et al. Mol Ther. 2025 Dec 24:S1525-0016(25)01061-5.

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