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CAS No.: 1374601-40-7

BRD4770 Catalog No. CSN13838

Synonyms: HMTase Inhibitor VI

BRD4770 is an inhibitor of histone methyltransferase G9a with IC50 of 6.3 μM and it can induce cell senescence.

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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].
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

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
- 2.4186 mL
- 12.0928 mL
- 24.1856 mL
- 5 mM
- 0.4837 mL
- 2.4186 mL
- 4.8371 mL
- 10 mM
- 0.2419 mL
- 1.2093 mL
- 2.4186 mL

技术信息

CAS号

1374601-40-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H23N3O3

运输

蓝冰

分子量

413.47

别名

HMTase Inhibitor VI

溶解度

DMSO	82.0 mg/mL (198.3 mM)
Water	insoluble

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