RGFP966, ≥98%
Product Name： RGFP966
CAS號:1357389-11-7
分子式:C21H19FN4O
分子量:362.4
貯存： 儲存溫度-20°C
可溶性： 25°C： DMSO
生化和生理學(xué)機(jī)理：
Description：
IC50 Value： 80 nM [1]
RGFP966 is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM.
in vitro： A titration of RGFP966 showed that at 5-10 ?M there was only a modest affect on H3K56ac, which was approximately 15-fold less than found with Depsipeptide. Treatment of two CTCL cell lines, HH and Hut78, with the HDAC3-selective inhibitors 966 and 136, for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac (even at 10?M) [2].
in vivo： To investigate the concentration of RGFP966 in the brain, we treated mice with 10 mg/kg RGFP966 administered s.c., then collected plasma and brain tissue at 15, 30, 60, and 120 min after treatment and analyzed the samples for drug levels. The maximum drug concentration (Cmax) in the brain was 1.25 ?g/g (3.15 ?M) at 30 min. RGFP966 concentration remained high up to 60 min and then declined significantly by 120 min [F(3,16) = 14.48,P < 0.001; Bonferroni post hoc： 30 min vs. 120 min, P < 0.05], but was still 0.57 ?g/g (1.5 ?M) [1].
Toxicity： N/A
Clinical trial： Preclinical
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