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CAS No.: 910462-43-0

Domatinostat Catalog No. CSN18556

Synonyms: 4SC-202 free base;4SC-202;domatinostat

Domatinostat is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

规格	价格	促销价格	库存	数量

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC1

IC50:1.20μM HDAC10

IC50:21μM HDAC11

IC50:9.7μM HDAC2

IC50:1.12μM HDAC3

IC50:0.57μM 更多
描述Domatinostat is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). In HeLa cells, Domatinostat induces hyperacetylation of histone H3 with EC₅₀ of 1.1 μM. Domatinostat induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, Domatinostat shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC₅₀ of 0.7 μM.
动物研究
动物给药方法
Mice: min = 80 mg/kg^[1], max = 120 mg/kg^[2]
剂量
Mice: min = 80 mg/kg^[1] (p.o.), max = 120 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
动物给药方法	Mice: min = 80 mg/kg^[1], max = 120 mg/kg^[2]
剂量	Mice: min = 80 mg/kg^[1] (p.o.), max = 120 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Gruber W, Peer E, et al. Targeting class I histone deacetylases by the novel small molecule inhibitor 4SC-202 blocks oncogenic hedgehog-GLI signaling and overcomes smoothened inhibitor resistance. Int J Cancer. 2018;142(5):968-975.
[2] S.W.Henning, R.Doblhofer, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2346 mL
- 11.1729 mL
- 22.3459 mL
- 5 mM
- 0.4469 mL
- 2.2346 mL
- 4.4692 mL
- 10 mM
- 0.2235 mL
- 1.1173 mL
- 2.2346 mL

技术信息

CAS号

910462-43-0

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H21N5O3S

运输

蓝冰

分子量

447.51

别名

4SC-202 free base;4SC-202;domatinostat

溶解度

DMSO	89 mg/ml (198.87 mM)
Water	Insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

10 mg/mL

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靶点	Description	IC50
HDAC1		IC50:1.20μM
HDAC10		IC50:21μM
HDAC11		IC50:9.7μM
HDAC2		IC50:1.12μM
HDAC3		IC50:0.57μM
HDAC9		IC50:50μM

Domatinostat Catalog No. CSN18556

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