HDAC2-IN-1

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HDAC2-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

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。

生物活性

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitiveHDAC2inhibitor with anIC₅₀of 0.5 μM^[1]. HDAC2-IN-1 also inhibitsHDAC1andHDAC8withIC₅₀s of 1.61 μM and 0.98 μM, respectively^[1].

IC₅₀& Target^[1]

HDAC2

0.5 μM (IC₅₀)

HDAC8

0.98 μM (IC₅₀)

HDAC1

1.61 μM (IC₅₀)

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

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.

分子量

426.96

Formula

C₂₂H₂₃ClN₄OS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.