HDAC2-IN-1 (Compound 17) 是一种能通过大脑屏障、具有口服活性、竞争性的HDAC2抑制剂，IC50为 0.5 μM。HDAC2-IN-1 也抑制HDAC1和HDAC8，IC50分别为 1.61 μM 和 0.98 μM。

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC 50 of 0.5 μM [1]. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC 50 s of 1.61 μM and 0.98 μM, respectively [1].

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 [1].

HDAC2-IN-1 (Compound 17) (30 or 100 mg/kg; p.o.; once) shows good plasma and brain exposure, and shows promising brain penetration [1]. Animal Model: Male C57BL/6 mice [1] Dosage: 30 or 100 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: Showed good plasma and brain exposure, also showed promising brain penetration, K p,uu = 0.36. Significantly increased histone H4K12 acetylation in mouse brain 4 h after oral dosing at 100 mg/kg.

C22H23ClN4OS

426.96

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years