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RGFP966

CAS No. : 1357389-11-7

MCE 国际站：RGFP966

产品活性：RGFP966 是高选择性的 HDAC3 抑制剂，IC₅₀ 为 80 nM，在 15 μM 时对其他 HDAC 无抑制作用。RGFP966 能够透过血脑屏障 (BBB)。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

In Vitro: RGFP966 potently and selectively inhibits HDAC 3 with IC₅₀ of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC₅₀=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered.

In Vivo: RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex.

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