1. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease
  2. HDAC MMP HIF/HIF Prolyl-Hydroxylase
  3. HNHA

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.

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HNHA Chemical Structure

HNHA Chemical Structure

CAS No. : 926908-04-5

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Based on 1 publication(s) in Google Scholar

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Description

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

 

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

303.42

Formula

C17H21NO2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NO)CCCCCCSC1=CC=C2C=CC=CC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (329.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2958 mL 16.4788 mL 32.9576 mL
5 mM 0.6592 mL 3.2958 mL 6.5915 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2958 mL 16.4788 mL 32.9576 mL 82.3940 mL
5 mM 0.6592 mL 3.2958 mL 6.5915 mL 16.4788 mL
10 mM 0.3296 mL 1.6479 mL 3.2958 mL 8.2394 mL
15 mM 0.2197 mL 1.0986 mL 2.1972 mL 5.4929 mL
20 mM 0.1648 mL 0.8239 mL 1.6479 mL 4.1197 mL
25 mM 0.1318 mL 0.6592 mL 1.3183 mL 3.2958 mL
30 mM 0.1099 mL 0.5493 mL 1.0986 mL 2.7465 mL
40 mM 0.0824 mL 0.4120 mL 0.8239 mL 2.0599 mL
50 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6479 mL
60 mM 0.0549 mL 0.2746 mL 0.5493 mL 1.3732 mL
80 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0299 mL
100 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8239 mL
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Help & FAQs
  • 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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