Top/HDAC-IN-2

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Top/HDAC-IN-2 

Top/HDAC-IN-2 (45b) 是一种 TopHDAC 的双重抑制剂,具有强大的抗肿瘤活性并诱导细胞凋亡

Top/HDAC-IN-2

Top/HDAC-IN-2 Chemical Structure

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生物活性

Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis[1].

IC50 & Target

HDAC1

0.004 μM (IC50)

HDAC2

0.005 μM (IC50)

HDAC3

1.10 μM (IC50)

HDAC6

0.15 μM (IC50)

HDAC8

4.5 μM (IC50)

Top1

 

Topoisomerase II

 

体外研究
(In Vitro)

Top/HDAC-IN-2 (45b) shows antitumor activities against the HCT116 (IC50 = 0.23 µM), MCF-7 and A549 cells[1].
Top/HDAC-IN-2 (45b) (0-5 µM, 24h) arrests the HCT116 cell cycle at the G2 phase in a concentration-dependent manner[1].
Top/HDAC-IN-2 (45b) (0-2.5 µM, 24h) induces the apoptosis in HCT116 cell line in a concentration-dependent manner[1].
Top/HDAC-IN-2 (45b) (0-5 μM, 24h) inhibits HDAC in living cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 0.1, 2.5 and 5 μM
Incubation Time: 24 h
Result: Arrested the HCT116 cell cycle at the G2 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 0.1, 0.5 and 2.5 μM
Incubation Time: 24 h
Result: Effectively induced the apoptosis in HCT116 cell line in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 1 μM and 5 μM
Incubation Time: 24 h
Result: Concentration-dependently increased the level of acetyl-H3 and acetyl-H4 in HCT116 cells.

分子量

568.63

Formula

C30H32N8O4

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.

参考文献
  • [1]. Fugui Zhu, et al. Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors. Bioorg Chem. 2022 May;122:105702.

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