1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. HDAC2-IN-3

HDAC2-IN-3 是一种选择性的、口服有效的、可穿过血脑屏障的 HDAC2 抑制剂,其 IC50 为 14 nM。HDAC2-IN-3 可在细胞及体内上调组蛋白乙酰化水平,增强海马体长时程增强效应 (LTP)。HDAC2-IN-3 可用于阿尔茨海默病的研究。

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HDAC2-IN-3

HDAC2-IN-3 Chemical Structure

CAS No. : 2652579-44-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC2-IN-3 is a selective, orally active, blood-brain barrier permeable HDAC2 inhibitor with an IC50 of 14 nM. HDAC2-IN-3 upregulates histone acetylation levels in cells and in vivo, and enhances long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

HDAC2

14 nM (IC50)

体外研究
(In Vitro)

HDAC2-IN-3 (Compound 11) (0.01-25.3 μM; 24 h) 可提高 C57B6J 小鼠胚胎原代皮质神经元中 H4K12 的乙酰化水平,最大作用效果达 71%,其 IC20 为 0.259 μM[1]
HDAC2-IN-3 (0.0411-83.3 μM; 过夜) 在 HDAC2-KO K562 细胞中对 HDAC1 的活性较低,与阳性对照相比,H3K9 乙酰化水平最高仅升高 12%[1]
HDAC2-IN-3 (0.1-25 μM; 48 h) 对人骨髓 CD34+祖细胞未表现出显著细胞毒性,在浓度高达 25 μM 时,其 IC50 > 25 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

HDAC2-IN-3 (Compound 11) (50 mg/kg;口服;单次给药) 可使 APP/PS1 小鼠海马区 H4K12 乙酰化水平升高至溶媒对照组的 ~220%,证实其在体内可抑制 HDAC2[1]
HDAC2-IN-3 (50 mg/kg;口服;每日一次;连续 10 天) 可显著增强 6 至 7 月龄 APP/PS1 小鼠的海马体 LTP,提示其具有改善学习与记忆形成的潜力[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: APP/PS1 (male; transgenic model generated by crossing Tg2576 mice with heterozygous PSEN1I213T KI mice)[1]
Dosage: 50 mg/kg
Administration: p.o.; single dose
Result: Elevated hippocampal H4K12 acetylation levels to approximately 220% of vehicle-treated control levels.
Animal Model: APP/PS1 (6- to 7-month-old; transgenic model generated by crossing Tg2576 mice with heterozygous PSEN1I213T KI mice)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 10 days
Result: Significantly enhanced hippocampal LTP compared to vehicle-treated mice, with a statistically significant difference observed in the field excitatory postsynaptic potential slope following theta burst stimulation.
分子量

376.43

Formula

C19H16N6OS

CAS 号
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.

纯度 & 产品资料
参考文献
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产品名称:
HDAC2-IN-3
目录号:
HY-182321
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