|N-(2-氨基苯基)吡嗪-2-甲酰胺|CsnPharm

CAS No.: 926259-99-6

BG45 Catalog No. CSN17264

Synonyms: BG45

BG45 is a selective inhibitor for HDAC3 with IC50 of 289 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述BG45 is a selective HDAC3 with IC50 value of 289nM. It triggered significant MM cell growth inhibition via apoptosis at 15μM post 48h, shown by caspase and PARP cleavage. BG45 at 10μM or 20μM in a dose-dependent fashion significantly induced acetylation of histone H2A, H3, and H4 (Ac-H3K9, Ac-H4K8, Ac-H4K12, Ac-H2AK5), reduced IL-6-induced p-STAT3-Y705, and triggered hyperacetylation of STAT3 at 20μM in MM.1S cells. Administration of BG45 at dose of 15mg/kg or 50mg/kg, i.p., 5 days a week for 3 weeks, significantly inhibited tumor growth in a murine xenograft model of human MM, and potentiated bortezomib-induced cytotoxicity in vivo^[2].
动物研究
剂量
Mice: 15 mg/kg, 50 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 15 mg/kg, 50 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Minami J, Suzuki R, et al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.
[2] Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KC. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9. doi: 10.1038/leu.2013.231. Epub 2013 Aug 5. PMID: 23913134; PMCID: PMC4165599.

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
- 4.6680 mL
- 23.3401 mL
- 46.6803 mL
- 5 mM
- 0.9336 mL
- 4.6680 mL
- 9.3361 mL
- 10 mM
- 0.4668 mL
- 2.3340 mL
- 4.6680 mL

技术信息

CAS号

926259-99-6

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

C11H10N4O

运输

蓝冰

分子量

214.22

别名

BG45

溶解度

DMSO	67.0 mg/mL (312.8 mM) warming
Water	insoluble

动物实验配方

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BG45 Catalog No. CSN17264

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