产品
编 号:F756854
分子式:C22H23ClN4OS
分子量:426.96
产品类型
结构图
CAS No: 2919691-32-8
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产品详情
生物活性:
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively.
体内研究:
HDAC2-IN-1 (Compound 17) (30 or 100 mg/kg; p.o.; once) shows good plasma and brain exposure, and shows promising brain penetration.Animal Model:Male C57BL/6 mice
Dosage:30 or 100 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Showed good plasma and brain exposure, also showed promising brain penetration, Kp,uu = 0.36. Significantly increased histone H4K12 acetylation in mouse brain 4 h after oral dosing at 100 mg/kg.
体外研究:
HDAC2-IN-1 (Compound 17) (3 and 10 μM; 48 h) increases histone H4K12 and H3K9 acetylation levels in SKNSH cells in a dose-dependent manner.