1. NF-κB
  2. NF-κB

NSC 80687 (Synonyms: Techtochrysin; Techtochrysine; Tectochrysin)

Cat. No.: HY-14592
Handling Instructions

NSC 80687 is one of the major flavonoids of Alpinia oxyphylla Miquel. NSC 80687 inhibits activity of NF-κB.

For research use only. We do not sell to patients.

NSC 80687 Chemical Structure

NSC 80687 Chemical Structure

CAS No. : 520-28-5

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Description

NSC 80687 is one of the major flavonoids of Alpinia oxyphylla Miquel. NSC 80687 inhibits activity of NF-κB.

IC50 & Target[1]

p50

 

p65

 

In Vitro

NSC 80687 (Tectochrysin) inhibits activity of NF-κB. NSC 80687 binds directly to the p50 unit. NSC 80687 concentration-dependently inhibits the translocation of p50 and p65 into the nucleus through inhibition of the phosphorylation of IκB. To assess the inhibitory effect of NSC 80687 (Tectochrysin) on cell growth of colon cancer cells (SW480, HCT116), cell viability is analyzed by MTT assay. The cells are treated with varying concentrations of NSC 80687 (1, 5, 10 μg/mL) for 24 h. NSC 80687 inhibits cell growth in colon cancer cells in a concentration-dependent manner. NSC 80687 inhibits SW480 cells growth with IC50 value of 6.3 μg/mL and HCT116 cells growth with IC50 value of 8.4 μg/mL. Morphologic observation shows that the cells are reduced in size by the treatment of NSC 80687 (10 μg/mL) in SW480 cells and HCT116 cells. However, NSC 80687 is not cytotoxic in the normal CCD-18co cells in the tested concentration by MTT assay. To delineate whether the induction of apoptotic cell death is critical for cell growth inhibition by NSC 80687, changes are evaluated in the chromatin morphology of cells using DAPI staining. To further characterize the apoptotic cell death by NSC 80687, TUNEL staining assays are performed, and then the labeled cells are analyzed by fluorescence microscopy. Apoptotic cells number (DAPI-positive TUNEL stained cells) in SW480 cell is increased to 1 and 58 % by 0 and 10 μg/mL NSC 80687, respectively, and 1 and 54 % by 0 and 10 μg/mL NSC 80687 in HCT116[1].

In Vivo

To elucidate the antitumor effects of NSC 80687 (Tectochrysin) in in vivo, the tumor growth in colon cancer xenograft-bearing nude mice following NSC 80687 treatments is investigated. In HCT116 xenograft studies, NSC 80687 is administrated i.p. twice per week for 3 weeks to mice with tumors ranging from 200 to 300 mm3 in volume. The mice are weighed twice per week. The changes in body weights between the control and the NSC 80687-treated mice (n=10) are not remarkably different during the experiment. However, On day 21, the final tumor weights are recorded. Tumor weights and volumes in mice treated with NSC 80687 at 5 mg/kg doses are 57.9 % and 46.4 % of the vehicle group, respectively[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7277 mL 18.6386 mL 37.2773 mL
5 mM 0.7455 mL 3.7277 mL 7.4555 mL
10 mM 0.3728 mL 1.8639 mL 3.7277 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Each SW480, HCT116, HT-29, A549 and MCF-7 cell line (1×104 cells) is incubated in 200 μL of RPMI 1640, DMEM medium with NSC 80687 (concentrations ranging from 1, 5, 10 μg/mL) in a 96-well flat-bottomed plate in triplicate. After incubation for 72 h at 37°C, MTT diluted in RPMI 1640, DMEM medium are added to each well and incubation is carried out for 90 min. The supernatant is then discarded and the crystal products are eluted with DMSO (200 μL/well). Colorimetric evaluation is performed with a spectrophotometer at 540 nm. The apoptosis assay is first performed by using DAPI staining. SW480 and HCT116 human colon cancer cells are cultured with concentrations of NSC 80687 (5 μg/mL), and induction of apoptotic cell death is evaluated after 24 h. Tunel assay is done[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Five-week-old male BALB/c athymic nude mice (n=10/group) are used. HCT116 cancer cells are injected subcutaneously (1×107 cells/0.1 mL PBS/animal) into the lower right flanks of mice. After 14 days, when the tumors have reached an average volume of 200-300 mm3, the tumor-bearing nude mice are intraperitoneally injected with NSC 80687 (5 mg/kg dissolved in 0.1 % DMSO) twice per week for 3 weeks. The tumor volumes are measured with vernier calipers and calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

268.26

Formula

C₁₆H₁₂O₄

CAS No.

520-28-5

SMILES

OC1=C2C(OC(C3=CC=CC=C3)=CC2=O)=CC(OC)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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NSC 80687
Cat. No.:
HY-14592
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NSC 80687

Cat. No.: HY-14592