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HDAC-IN-47
本半岛bd体育手机客户端 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。
HDAC-IN-47图片
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
HDAC-IN-47 是一种具有口服活性的组蛋白去乙酰化酶 ( HDAC) 的抑制剂， IC50分别为 19.75 nM ( HDAC1)，5.63 nM ( HDAC6)，40.27 nM ( HDAC3)，57.8 nM ( HDAC2)，302.73 nM ( HDAC8)。HDAC-IN-47 能抑制细胞自噬，并通过 Bax/Bcl-2和 caspase-3通路诱导凋亡 ( apoptosis)。HDAC-IN-47 能够在G2/M期阻滞细胞周期，并在体内表现出抗肿瘤作用。
生物活性

HDAC-IN-47 is an orally active inhibitor ofhistone deacetylase(HDAC), withIC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibitsautophagyand inducesapoptosisvia theBax/Bcl-2andcaspase-3pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo[1].
IC50& Target[1]

HDAC1

19.75 nM (IC50)

HDAC6

5.63 nM (IC50)

HDAC3

40.27 nM (IC50)

HDAC2

57.8 nM (IC50)

HDAC8

302.73 nM (IC50)
体外研究
(In Vitro)

HDAC-IN-47 (compound 21) shows antiproliferative activity and inhibits A549 cell growth with an IC50value of 0.24 μM[1].
HDAC-IN-47 (0.5 and 1 μM; 72 h) exhibits profound G2/M arrest in A549 cells and induces cell apoptosis[1].
HDAC-IN-47 (0.1 and 0.5 μM; 24 h) increases the expression levels of Bax and Caspase3, decreases the level of Bcl-2, activates the intrinsic (mitochondrial) apoptotic pathway[1].

Cell Viability Assay[1]

Cell Line: HepG2, MDA-MB-238, HL-60 cells
Concentration: 0.16-0.45 μM
Incubation Time: 72 hours
Result: Inhibited cancer cells with IC50s of 0.16 μM (HepG2), 0.45 μM (MDA-MB-238), 0.22 μM (HL-60), respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Induced marked arrest of cells in the G2/M phase of 28.38% (0.5 μM) and 31.70% (1.0 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Resulted 21.09% (0.5 μM) and 30.58% (1 μM) apoptotic cells.
体内研究
(In Vivo)

HDAC-IN-47 (compound 21) (50, and 100 mg/kg; p.o.; once daily; 18 d) exhibits significant antitumor activity in a dosedependent manner without no significant body weight loss in A549 xenograft mouse model[1].

Animal Model: A549 xenograft model in mouse (female, BALB/c nu/nu mice, 6-8 weeks old)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: Oral gavage; once daily; for 18 consecutive days
Result: Decreased the tumor volume and weight by 48% and 45%, respectively.
分子量

410.26
Formula

C17H20BrN3O4
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.
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