GXH-II-052

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GXH-II-052

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

GXH-II-052 是一种有效的二价BET（bivalent bromodomain and extraterminal domain (BET)）抑制剂。GXH-II-052 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 28、9.1、4.8、0.6、8.4、2.6 nM。GXH-II-052 显示出抗增殖活性。GXH-II-052 降低 c-Myc 的表达。

生物活性

GXH-II-052 is a potentbivalent bromodomain and extraterminal domain (BET)inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T withK_dvalues of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression ofc-Myc^[1].

IC₅₀& Target^[1]

BRD4-1

28 nM (Kd)

BRD4-2

9.1 nM (Kd)

BRD4-T

4.8 nM (Kd)

BRDT-1

0.6 nM (Kd)

BRDT-2

8.4 nM (Kd)

BRDT-T

2.6 nM (Kd)

体外研究
(In Vitro)

GXH-II-052 (0-10 μM; 72 h) shows antiproliferative activity with anIC₅₀value of 59 nM in MM1.S cells^[1].
GXH-II-052 (0-10 μM; 6 h) decreases the expression of c-Myc in a dose dependent manner^[1].

Cell Viability Assay^[1]

Cell Line:	MM1.S cells
Concentration:	0-10 μM
Incubation Time:	72 h
Result:	Showed growth inhibition with an IC₅₀value of 59 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)

GXH-II-052 shows metabolic stability in mouse and human liver microsomes with an T_1/2values of 33, 3.6 min, respectively^[1].

分子量

1366.39

Formula

C₆₂H₇₆Cl₂F₂N₁₄O₁₁S₂

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.