A2AAR/HDAC-IN-2

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A2AAR/HDAC-IN-2

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。

CAS NO:

2767560-94-9

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

A2AAR/HDAC-IN-2 是一种有效的A_2AAR/HDAC双重抑制剂，其对A_2AAR具有良好的亲和力 (K_i=10.3 nM), 对HDAC1具有良好的抑制活性 (IC₅₀=18.5 nM). A2AAR/HDAC-IN-2 可用于抗肿瘤的研究。

生物活性

A2AAR/HDAC-IN-2 is a potentA_2AAR/HDACdual inhibitor, with good binding affinity forA_2AAR(K_i=10.3 nM) and good inhibitory activity againstHDAC1(IC₅₀=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor^[1].

IC₅₀& Target

HDAC1

18.5 nM (IC₅₀)

HDAC2

16.0 nM (IC₅₀)

HDAC3

13.6 nM (IC₅₀)

HDAC6

2.1 nM (IC₅₀)

HDAC8

1408.9 nM (IC₅₀)

A1AR

105.6 nM (Ki)

A2AAR

10.3 nM (Ki)

A2BAR

513.0 nM (Ki)

A3AR

＞10 μM (IC₅₀)

体外研究
(In Vitro)

A2AAR/HDAC-IN-2 (compound 30c) (5 nM-100 μM; 72 h) shows anti-proliferative activity, with GI₅₀s of 12.16 and 12.61 μM for CT26 and MC38 cells, respectively^[1].
A2AAR/HDAC-IN-2 (0.1, 1, 5, 10 μM; 24 h) increases histone H3 and H4 acetylation in a concentration-dependent manner in MC38 cells^[1].

Cell Proliferation Assay^[1]

Cell Line:	MC38 and CT26 cells
Concentration:	5 nM-100 μM
Incubation Time:	72 h
Result:	Showed good anti-proliferative activity in cancer cell lines, with GI₅₀s of 12.16 and 12.61 μM for CT26 and MC38 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	MC38 cells
Concentration:	0.1, 1, 5, 10 μM
Incubation Time:	24 h
Result:	Significantly increases histone H3 and H4 acetylation at 10 μM and in a concentration-dependent manner.

分子量

450.49

Formula

C₂₃H₂₆N₆O₄

CAS 号

2767560-94-9

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.