HDAC-IN-9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HDAC-IN-9 

HDAC-IN-9 是一种有效的选择性 tubulin 和 HDAC 双重抑制剂。HDAC-IN-9 抑制 A549 细胞的侵袭和迁移。HDAC-IN-9 在体外和体内均显示出有效的抗肿瘤和抗血管生成作用。

HDAC-IN-9

HDAC-IN-9 Chemical Structure

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生物活性

HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo[1].

IC50 & Target[1]

HDAC1

6.8 μM (IC50)

HDAC2

0.06 μM (IC50)

HDAC6

0.12 μM (IC50)

HDAC8

8.5 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-9 (compound 4s) shows anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively)[1].
HDAC-IN-9 displays 6.1, 3.2 and 4.6-fold selectivity ratios for 293 T, macrophages, and L02 cells respectively (IC50s of 10.89, 5.63, 8.14 µM for 293 T, macrophages, and L02 cells, respectively)[1].
HDAC-IN-9 shows inhibition activities against HDAC isoforms (IC50s of 6.8, 0.06, 0.12, 8.5 µM for HDAC 1, HDAC 2, HDAC 6, HDAC 10, respectively)[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h; A459 cells) induces cell cycle arrest at the G2/M phase in a concentration-dependent manner[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h) induces apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells[1].
HDAC-IN-9 (0, 0.5, 1, 2 µM; 48 h) shows anti-proliferative activity by the inhibition of angiogenesis and the reduction of endothelial cell metastasis in A549 cells[1].
HDAC-IN-9 (0, 1, 2, 4 µM, 48 h) inhibits the invasion and migration of A549 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively).

Cell Cycle Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Cells were arrested at the G2/M phase with a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Induced apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells.

Western Blot Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Showed down regulation of Cyclin B1 and Pcdc2 levels.

体内研究
(In Vivo)

HDAC-IN-9 (0, 10, 20, 40 µM) suppresses the formation of intersegmental blood vessels (ISVs) in zebrafish embryos[1].
HDAC-IN-9 (0, 2.5, 5, 10 µM; 3 days) inhibits the proliferation and metastasis of A549 cells in zebrafish xenograft models[1].

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

Animal Model: embryos of Tg(flk:EGFP) transgenic zebrafish (transgenic zebrafish model Tg(flk1:EGFP))[1]
Dosage: 0, 10, 20, 40 µM
Administration:
Result: Suppressed the formation of ISVs in zebrafish embryos.
Animal Model: zebrafish xenograft models[1]
Dosage: 0, 2.5, 5, 10 µM
Administration: 3 days
Result: Inhibited the proliferation and metastasis of A549 cells in zebrafish xenograft models.

分子量

526.67

Formula

C33H38N2O4
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]. Sun M, et al. 2-Methoxydiol derivatives as new tubulin and HDAC dual-targeting inhibitors, displaying antitumor and antiangiogenic response. Bioorg Chem. 2022; 120:105625.

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