您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > NC-III-49-1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
NC-III-49-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NC-III-49-1图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
NC-III-49-1 是一种有效的二价BET(bivalent bromodomain and extraterminal domain (BET))抑制剂。NC-III-49-1 显示与 BRD4-1、BRD4-2、BRD4-T、BRDT-1、BRDT-2、BRDT-T 的结合潜力,Kd值分别为 0.095、0.32、0.29、0.089 、5.5、0.058 nM。NC-III-49-1 显示出抗增殖活性。NC-III-49-1 降低 c-Myc 的表达。
生物活性

NC-III-49-1 is a potentbivalent bromodomain and extraterminal domain (BET)inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T withKdvalues of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression ofc-Myc[1].

IC50& Target[1]

BRD4-1

0.095 nM (Kd)

BRD4-2

0.032 nM (Kd)

BRD4-T

0.29 nM (Kd)

BRDT-1

0.089 nM (Kd)

BRDT-2

5.5 nM (Kd)

BRDT-T

0.058 nM (Kd)

体外研究
(In Vitro)

NC-III-49-1 (0-10 μM; 72 h) shows antiproliferative activity with anIC50value of 0.69 nM in MM1.S cells[1].
NC-III-49-1 (0-10 μM; 6 h) decreases the expression of c-Myc in a dose dependent manner[1].
. NC-III-49-1 shows inhibition by interact with both KAc sites[1].

Cell Viability Assay[1]

Cell Line:MM1.S cells
Concentration:0-10 μM
Incubation Time:72 h
Result:Showed subnanomolar growth inhibition with an IC50value of 0.69 nM in multiple myeloma MM1.S cells.

Western Blot Analysis[1]

Cell Line:MM1.S cells
Concentration:0-10 μM
Incubation Time:6 h
Result:Decreased the expression of c-Myc in a dose dependent manner.
体内研究
(In Vivo)

NC-III-49-1 shows metabolic stability in human and mouse liver microsomes with an T1/2values of<2.3,<2.3 min, respectively[1].

分子量

875.02

Formula

C44H50N4O11S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.