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HNHA

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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。

HNHA 

HNHA 是一种有效的组蛋白去乙酰化酶 (HDAC)抑制剂。HNHA 通过 p21 诱导在 G1/S 期阻滞细胞周期。HNHA 可抑制肿瘤生长和抑制肿瘤新生血管形成。HNHA 可能是一种有效的抗乳腺癌剂。

HNHA

HNHA Chemical Structure

CAS No. : 926908-04-5

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生物活性

HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer[1].

IC50 & Target

MMP-2

 

MMP-9

 

体外研究
(In Vitro)

HNHA (0-100 μM, 96 h) shows strong inhibition at lower concentrations on cancer cell lines, especially on breast cancer cells, mouse FM3A and human MCF-7[1].
HNHA (15 μM, 24 h) arrests cancer cells at the G1/S phase of the cell cycle, activates p21and rescues strongly protein acetylation[1].
HNHA (15 μM, 12 h) inhibits angiogenic proteins in breast cancer cells, effectively inactivates MMP-2, MMP-9, VEGF and HIF-1α[1].

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

Cell Proliferation Assay

Cell Line: FM3A, C1300, LA-N-1, LA-N-2, LA-N-5, NB16, NB19, NB69, SK-N-SH, MCF-7 and HT-29[1]
Concentration: 0-100 μM
Incubation Time: 96 h
Result: Showed strong inhibition at lower concentrations on all cancer cell lines (FM3A, C1300, LA-N-1, LA-N-2, LA-N-5, NB16, NB19, NB69, SK-N-SH, MCF-7 and HT-29), with IC50 values of 15.70, 55.63, 22.78, 23.18, 26.70, 19.64, 21.26, 22.31, 65.09, 14.33, and 16.98 μM, respectively.

Cell Viability Assay

Cell Line: FM3A and MCF-7[1]
Concentration: 0, 0.1, 1, 5, 10, 15, 20, 25,30 μM
Incubation Time: 48 h
Result: Showed dose-dependent inhibition of viability in mouse and human breast cancer cells.

Cell Cycle Analysis

Cell Line: FM3A and MCF-7 cells[1]
Concentration: 15 μM
Incubation Time: 24 h
Result: Arrested FM3A and MCF-7 cells in the G1/S phase.

Western Blot Analysis

Cell Line: FM3A and MCF-7 cells[1]
Concentration: 0, 0.1, 1, 10, and 20 μM (24 h)
Incubation Time: 1, 6, 24, 48, and 72 h (15 μM)
Result: Activated a cell proliferation arrestor p21, increased histone and non-histone protein acetylation and inhibited FM3A and MCF-7 proliferation in vitro, and was very effective in increasing the acetylation level of histone H3 protein in FM3A and MCF-7. The most effective dose point for acetylation of histone H3 was 10-20 μM. Histone H3 acetylation peaked after 1 h of exposure to the drugs and remained stable for 1-6 h.

Western Blot Analysis

Cell Line: FM3A and MCF-7 cells[1]
Concentration: 15 μM
Incubation Time: 12 h
Result: Showed a strong induction of TIMP-1 and TIMP-2, and effectively inactivated MMP-2, MMP-9, VEGF and HIF-1α.

体内研究
(In Vivo)

HNHA (20 μM/mouse, IP, once every 2 days for a total of six injections) reduces tumor burden and extends the survival rate, activates TIMP-1, TIMP-2 and p21 and inhibits MMP-2, MMP-9, HIF-1α and VEGF protein expression[1].

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

Animal Model: C3H/HeJ-FasL mice (FM3A breast cancer cell tumor xenograft, 6 weeks, n = 25/group)[1]
Dosage: 20 μM/mouse
Administration: IP, once every 2 days for a total of six injections
Result: Reduced tumor burden and extended the survival rate. Effectively inhibited cancer development and angiogenesis in vivo. Increased TIMP-1, TIMP-2 and p21, decreased MMP-2, MMP-9, HIF-1α and VEGF protein expression, and reduced the distribution of CD34, HIF-1α and VEGF.

分子量

303.42

Formula

C17H21NO2S
CAS 号

926908-04-5
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]. Park KC, et al. Potential anti-cancer activity of N-hydroxy-7-(2-naphthylthio) heptanomide (HNHA), a histone deacetylase inhibitor, against breast cancer both in vitro and in vivo. Cancer Sci. 2011 Feb;102(2):343-50.

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