79-6 (CID5721353)

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规格或纯度 10mM in DMSO
货号(SKU) C423108
品牌 阿拉丁
  • 包装

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条款和条件
30天退款保证
运输:2-3 个工作日

规格


Cas Number 301356-95-6
规格或纯度 10mM in DMSO
包装 1ml

产品信息


品牌 阿拉丁
浓度 10mM in DMSO
简短描述 Bcl-6 抑制剂
英文简短描述 Bcl-6 Inhibitors
过滤标签 Compound libraries
储存温度 -80℃储存
运输条件 超低温冰袋运输
生化和生理学机理 79-6(CID5721353)(BCL6 抑制剂)是一种 BCL6 抑制剂,其 Kd 值为 138 μM。
英文描述

Information

79-6 (CID5721353) 79-6 (CID5721353) (BCL6 inhibitor) is a BCL6 inhibitor with Kd value of 138 μM.

Targets

Bcl-6 138 μM(Kd)

In vitro

Small molecular BCL6 inhibitor 79-6 is a cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 but does not affect BCL6 protein levels. 79-6 binds an aromatic pocket situated in the BTB domain lateral groove, induces disruption of BCL6 transcriptional complexes, reactivation of BCL6 target genes and selective killing of BCL6-dependent DLBCL cells. BCL6 can also interact with MTA3 through its RD2 domain and represses the terminal differentiation. It recruits CtBP through its DBD domain and represses its own expression. 79-6 suppresses invasive ability and colony-forming ability in both of MCF-7 and MDA231 cells. The inhibition of BCL6 with 79-6 enhanced the mRNA expression of E-cadherin in both of MCF-7 and MDA231 cells. 79-6 reverses the functions of BCL6 in the positive regulation of EMT, invasion and transcriptional repression of E-cadherin in breast cancer cells.

In vivo

Administration of 50 mg/kg/day 79-6 to SCID mice induced a 65-70% reduction in the size of established BCL6-dependent DLBCL xenografts, but had no effect on BCL6-independent DLBCLs. Therapeutic targeting of BCL6 with the small molecule 79-6 is an effective antilymphoma strategy in vivo.

Cell Research(from reference)

Cell lines:MCF-7 and MDA231 cells 

Concentrations:200 μM 

Incubation Time:48 h 

技术规格说明书


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