NC-III-49-1

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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。

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，K_d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 withK_dvalues 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 T_1/2values 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.