Bobcat339是一种高效且选择性的基于胞嘧啶的TET酶抑制剂,对TET1和TET2的IC50值分别为33 μM和73 μM。它在表观遗传学研究中具有重要价值,并作为开发针对DNA甲基化和基因转录的新治疗药物的起点。
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描述 | The TET (Ten-11 translocation methylcytosine dioxygenase) family of enzymes is known to be responsible for catalyzing the reverse process that is DNA demethylation by recognizing 5-methylcytosine and oxidizing the methyl group via an Fe(II)/alpha-ketoglutarate-dependent mechanism. Bobcat339 is a selective cytosine based TET enzyme inhibitor with IC50 values of 33 μM and 73 μM, respectively, for TET1 and TET2. HT-22 cells, an immortalized mouse hippocampal neuronal cell line, treated with 10 μM Bobcat339 for 24 h had significantly reduced global 5hmC levels as compared to the vehicle control, demonstrating its ability to reduce DNA 5hmC abundance by inhibiting TET enzyme function in living cells and providing support for its utility as a viable pharmacological probe[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.36mL 0.67mL 0.34mL |
16.79mL 3.36mL 1.68mL |
33.59mL 6.72mL 3.36mL |
CAS号 | 2280037-51-4 |
分子式 | C16H12ClN3O |
分子量 | 297.74 |
别名 | BC339 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
溶解方案 |
DMSO: 4 mg/mL(13.43 mM),配合低频超声,并水浴加热至45℃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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |