BG45

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Chemical Structure| 926259-99-6 同义名 : -
CAS号 : 926259-99-6
货号 : A304243
分子式 : C11H10N4O
纯度 : 99%+
分子量 : 214.223
MDL号 : MFCD09046162
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(233.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HDAC3

    HDAC3, IC50:289 nM

  • HDAC2

    HDAC2, IC50:2.2 μM

  • HDAC1

    HDAC1, IC50:2 μM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.67mL

0.93mL

0.47mL

23.34mL

4.67mL

2.33mL

46.68mL

9.34mL

4.67mL
参考文献

[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.