1. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage
  2. PI3K HDAC
  3. PI3K/HDAC-IN-2

PI3K/HDAC-IN-2 是一种有效的双重 PI3K/HDAC 抑制剂,对 PI3Kα、PI3Kβ、PI3Kγ、PI3Kδ的 IC50 分别为 226 nM、279 nM、467 nM、29 nM,对于 HDAC1、HDAC2、HDC4、HDAC6、HDAC8,IC50 分别为 1.3 nM、3.4 nM、972 nM、17 nM、12 nM。PI3K/HDAC-IN-2 表现出 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性。PI3K/HDAC-IN-2具有显着的抗癌作用。

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PI3K/HDAC-IN-2 Chemical Structure

PI3K/HDAC-IN-2 Chemical Structure

CAS No. : 2361418-65-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].

IC50 & Target[1]

PI3Kα

226 nM (IC50)

PI3Kβ

279 nM (IC50)

PI3Kγ

467 nM (IC50)

PI3Kδ

29 nM (IC50)

HDAC1

1.3 nM (IC50)

HDAC2

3.4 nM (IC50)

HDAC4

972 nM (IC50)

HDAC6

17 nM (IC50)

HDAC8

12 nM (IC50)

体外研究
(In Vitro)

For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively[1].
PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

461.47

Formula

C23H23N7O4

CAS 号
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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PI3K/HDAC-IN-2
目录号:
HY-146159
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