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HDAC-IN-47
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。
HDAC-IN-47图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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-2caspase-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.