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

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 HDAC1HDAC8IC50 分别为 1.61 μM 和 0.98 μM。

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HDAC2-IN-1 Chemical Structure

HDAC2-IN-1 Chemical Structure

CAS No. : 2919691-32-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1]. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s 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].

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

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].

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

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, Kp,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

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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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HDAC2-IN-1
目录号:
HY-151248
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