质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
创始人
GlaxoSmithKline
相关疾病
cancer
储存温度
2-8°C
InChI
1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1
InChI key
VUVUVNZRUGEAHB-CYBMUJFWSA-N
应用
GSK1210151A 或 I-BET151 已用于研究其在治疗 MLL（混合谱系白血病）-融合性白血病中对 BET（溴结构域和额外末端）募集染色质的抑制作用。
生化/生理作用
GSK1210151A（I-BET151）是 BET（溴结构域和额外末端域蛋白）家族的乙酰赖氨酸识别染色质 ′衔接子′ 蛋白抑制剂。GSK1210151A 取代了染色质的 BRD3 和 BRD4、PAFc 和 SEC 组份，从而抑制了参与混合谱系白血病（MLL）的关键基因（BCL2、C-MYC 和 CDK6）的转录。GSK1210151A（I-BET151）在 2 个 MLL 动物模型中显示出良好的疗效。
其他说明
化学探针门户网站已对 GSK1210151A 进行了专家评审和推荐。欲了解更多信息，请访问化学探针门户网站上的 GSK1210151A 探针摘要 。
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Replication Study: Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Shan X, et al.
eLife, 6, e25306-e25306 (2017)
Zhongyuan Gao et al.
Cancer biology & therapy, 19(5), 407-415 (2018-01-16)
Lung cancer is the leading cause of cancer-related death worldwide. Bromodomain and extraterminal domain (BET) proteins act as epigenome readers for gene transcriptional regulation. Among BET family members, BRD4 was well studied, but for its mechanism in non-small cell lung
Lisa-Maria Winter et al.
Scientific reports, 13(1), 12061-12061 (2023-07-27)
GDF15 has recently emerged as a key driver of the development of various disease conditions including cancer cachexia. Not only the tumor itself but also adverse effects of chemotherapy have been reported to contribute to increased GDF15. Although regulation of
Jun Li et al.
Cell reports, 37(11), 110124-110124 (2021-12-16)
Regulatory T (Treg) cells play crucial roles in suppressing deleterious immune response. Here, we investigate how Treg cells are mechanistically induced in vitro (iTreg) and stabilized via transcriptional regulation of Treg lineage-specifying factor Foxp3. We find that acetylation of histone tails
Yan-Yi Jiang et al.
Gastroenterology, 159(4), 1311-1327 (2020-07-04)
We investigated the transcriptome of esophageal squamous cell carcinoma (ESCC) cells, activity of gene regulatory (enhancer and promoter regions), and the effects of blocking epigenetic regulatory proteins. We performed chromatin immunoprecipitation sequencing with antibodies against H3K4me1, H3K4me3, and H3K27ac and
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