BRD4770

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Chemical Structure| 1374601-40-7 同义名 : HMTase Inhibitor VI
CAS号 : 1374601-40-7
货号 : A440833
分子式 : C25H23N3O3
纯度 : 99%+
分子量 : 413.47
MDL号 : MFCD23143627
存储条件：

Pure form Sealed in dry, 2-8°C

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

DMSO: 35 mg/mL(84.65 mM)，配合低频超声助溶，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
生物活性
靶点

  • Histone Methyltransferase
描述 Somatic mutation and amplification of histone methyltransferases are commonly observed in human cancers. BRD4770 is a selective, small-molecule inhibitor of histone methyltransferase G9a. The IC50 value of its active form (BRD9539) for G9a activity in cells is 6.3μM. Treatment of PANC-1 cells with 10μM BRD4770 for 24 hours resulted in a significant decrease in di- and trimethylation levels of H3K9, as well as an increase in monomethylation level. Treatment of PANC-1 cells with 5μM BRD4770 for 24 hours decreased trimethylation level of H3K9 by 23%. The EC50 values of BRD4770 for trimethylated H3K9 in PANC-1 cells were ~5μM. BRD4770-treated PANC-1 cells also showed increased cell population in G2/M and decreased G0/G1 cell fraction compared with DMSO-treated controls[3]. The subcutaneous injection of BRD4770 (10mg/kg, three times per week on days 1, 3, and 5) combined with prexasertib (2mg/kg, injection for three days followed by four-day off) inhibited the growth of subcutaneous L3.6 xenografts in mice[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.09mL

2.42mL

1.21mL

24.19mL

4.84mL

2.42mL
参考文献

[1]Yuan Y, Tang AJ, et al. Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. Cell Death Dis. 2013 Jun 27;4:e690.

[2]Yuan Y, Wang Q, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.

[3]Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp MM, Adams DJ, Shamji AF, Wagner BK, Schreiber SL. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7

[4]Urrutia G, Salmonson A, Toro-Zapata J, de Assuncao TM, Mathison A, Dusetti N, Iovanna J, Urrutia R, Lomberk G. Combined Targeting of G9a and Checkpoint Kinase 1 Synergistically Inhibits Pancreatic Cancer Cell Growth by Replication Fork Collapse. Mol Cancer Res. 2020 Mar;18(3):448-462