|3-(1-乙酰基-5-甲氧基-1H-吲哚-3-甲酰胺基)-4-氟苯甲酸叔丁酯|CsnPharm

CAS No.: 2443789-32-8

CBP/p300-IN-1 Catalog No. CSN27738

CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述CBP and p300 are highly homologous coactivators which promote gene transcription by bridging between DNA-binding transcription factors and the basal transcription machinery, by providing a scaffold for integrating transcription factors, and by modifying transcription factors and chromatin through acetylation^[2]. CBP/p300-IN-1 is a CBP/EP300 bromodomain (BRD) inhibitor（BDIs）^[1]. The presence of amyloid-like aggregates coincides with increased cytotoxicity, and cell viability can be restored upon co-treating cells with small-molecule p300/CBP BDIs, which reflect reduced levels of protein aggregates. p300/CBP BDIs impede aggregation, which coincides with enhanced UPS function and increased cell viability^[3]. CBP/EP300 bromodomain inhibition decreases somatic-specific gene expression, histone H3 lysine 27 acetylation (H3K27Ac) and chromatin accessibility at target promoters and enhancers. The master mesenchymal transcription factor PRRX1 is one such functionally important target of CBP/EP300 bromodomain inhibition^[4]. In preclinical tumor models, in vivo administration of a CBP/EP300-BRD inhibitor (CBP/EP300-BRDi) alters intratumoral MDSCs and attenuates established tumor growth in immunocompetent tumor-bearing mice, as well as in MDSC-dependent xenograft models. Inhibition of CBP/EP300-BRD redirects tumor-associated MDSCs from a suppressive to an inflammatory phenotype through downregulation of STAT pathway-related genes and inhibition of Arg1 and iNOS. Similarly, CBP/EP300-BRDi decreases differentiation and suppressive function of human MDSCs in vitro^[5].
参考文献

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
- 2.3450 mL
- 11.7250 mL
- 23.4501 mL
- 5 mM
- 0.4690 mL
- 2.3450 mL
- 4.6900 mL
- 10 mM
- 0.2345 mL
- 1.1725 mL
- 2.3450 mL

技术信息

CAS号	2443789-32-8	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H23FN2O5	运输	蓝冰
分子量	426.44	别名

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

CBP/p300-IN-1 Catalog No. CSN27738

靶点选择性

请登录您的专属账户

确认信息