1. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein Apoptosis
  2. Tyrosinase Ras Raf MAPKAPK2 (MK2) Apoptosis
  3. Norartocarpetin

Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells.

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Norartocarpetin Chemical Structure

Norartocarpetin Chemical Structure

CAS No. : 520-30-9

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Description

Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells[1][2].

IC50 & Target

IC50: 0.47 μM (tyrosinase);[1] IC50: 22 μM (NCI-H460 cells); 85 μM (MRC-9 cells)[2]

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
60.6 μM
Compound: 1
Inhibition of human recombinant BACE-1 expressed in HEK293 cells assessed as inhibition of amyloid precursor protein cleavage into amyloid beta after 60 mins using Rh-EVNLDAEFK-Quencher as a substrate by FRET assay
Inhibition of human recombinant BACE-1 expressed in HEK293 cells assessed as inhibition of amyloid precursor protein cleavage into amyloid beta after 60 mins using Rh-EVNLDAEFK-Quencher as a substrate by FRET assay
[PMID: 21511472]
In Vitro

Norartocarpetin has strong mushroom tyrosinase inhibitory activity with an IC50 value of 0.47 μM[1].
Norartocarpetin (0-100 μM; 48 h) leds to dose-dependent cytotoxic effects in NCI-H460 cells and MRC-9 cells with IC50 values of 22 μM and 85 μM, respectively[2].
Norartocarpetin (0, 11, 22, and 44 μM; 24 h) led to blockade of Ras/Raf/MAPK signalling pathway[2].
Norartocarpetin (0, 11, 22, and 44 μM, 24 h) induced the apoptosis of the human lung carcinoma cells (NCI-H460)[2].
Norartocarpetin (0, 11, 22, and 44 μM) leds to S-phase cell cycle arrest[2].
Norartocarpetin (22 μM; 24 h) leds to dose-dependent suppression of cell invasion[2].
Norartocarpetin (0, 11, 22, and 44 μM, 24 h) leds to significant inhibition of cell migration[2].

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

Cell Viability Assay[2]

Cell Line: MRC-9 (normal fibroblast lung cells) and NCI-H460 (human lung cancer cells)
Concentration: 0, 3.12, 6.25, 12.5, 25, 50, and 100 μM
(first dissolved in DMSO at 1.0 mg/mL and then diluted to different concentrations using DMSO, 30 μL, 20min)
Incubation Time: 48 h
Result: Repressed the viability of NCI-H460 cells in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: MRC-9 and NCI-H460 cells
Concentration: 0, 11, 22, and 44 μM
Incubation Time: 24 h
Result: Significantly reduced the expression of p-RAS, p-RAF and p-P38 and unchanged the expressions of RAS, RAF and P38.

Apoptosis Analysis[2]

Cell Line: MRC-9 and NCI-H460 cells
Concentration: 0. 11, 22 and 44 μM
Incubation Time: 24 h
Result: Led to dose-dependent apoptosis and induced DNA damage.

Cell Cycle Analysis[2]

Cell Line: MRC-9 and NCI-H460 cells
Concentration: 0, 11, 22, and 44 μM
Incubation Time:
Result: Showed increase of S-phase cells and the percentage of S-phase NCI-H460 LC cells was 30%, 40%, 55% and 70% at 0, 11, 22 and 44 μM concentrations, respectively.

Cell Invasion AssayMRC-9 and NCI-H460 cells

Cell Line: MRC-9 and NCI-H460 cells
Concentration: 22 μM
Incubation Time: 24 h
Result: Significantly reducted (from 100% to about 40%) in the invasion of NCI-H460 human LC cells.

Cell Migration Assay [2]

Cell Line: MRC-9 and NCI-H460 cells
Concentration: 0, 11, 22, and 44 μM
Incubation Time: 24 h
Result: Decreased remarkably the cell invasion in NCI-H460 LC cells in a concentration- dependent manner.
Molecular Weight

286.24

Formula

C15H10O6

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1C=C(C2=CC=C(O)C=C2O)OC3=CC(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (349.36 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 3.4936 mL 17.4679 mL 34.9357 mL
5 mM 0.6987 mL 3.4936 mL 6.9871 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 (protect from light). 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

Purity: 98.92%

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 (protect from light). 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 3.4936 mL 17.4679 mL 34.9357 mL 87.3393 mL
5 mM 0.6987 mL 3.4936 mL 6.9871 mL 17.4679 mL
10 mM 0.3494 mL 1.7468 mL 3.4936 mL 8.7339 mL
15 mM 0.2329 mL 1.1645 mL 2.3290 mL 5.8226 mL
20 mM 0.1747 mL 0.8734 mL 1.7468 mL 4.3670 mL
25 mM 0.1397 mL 0.6987 mL 1.3974 mL 3.4936 mL
30 mM 0.1165 mL 0.5823 mL 1.1645 mL 2.9113 mL
40 mM 0.0873 mL 0.4367 mL 0.8734 mL 2.1835 mL
50 mM 0.0699 mL 0.3494 mL 0.6987 mL 1.7468 mL
60 mM 0.0582 mL 0.2911 mL 0.5823 mL 1.4557 mL
80 mM 0.0437 mL 0.2183 mL 0.4367 mL 1.0917 mL
100 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8734 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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Norartocarpetin
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