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Reagents and instruments for immunology, cell biology and molecular biology.

Nobiletin [478-01-3]

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Cat# HY-N0155-5mg

Size : 5mg

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Brand : MedChemExpress

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Description

Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis^[1]^[2]^[3]^[4].

IC₅₀ & Target

Retinoid acid receptor-related orphan receptors (RORs)^[1]; reactive oxygen species (ROS)^[1]; apoptosis^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	36.53 μM Compound: 44	Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay	[PMID: 36459083]
DU-145	IC₅₀	144.5 μM Compound: 44	Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay	[PMID: 36459083]
HL-60	IC₅₀	10 ng/mL Compound: Nobiletin	Growth inhibition of human HL60 cells after 72 hrs by MTT assay Growth inhibition of human HL60 cells after 72 hrs by MTT assay	[PMID: 31398616]
HL-60	IC₅₀	41.5 μM Compound: I	Antiproliferative activity against HL60 after 24 hrs Antiproliferative activity against HL60 after 24 hrs	[PMID: 17391969]
HT-29	IC₅₀	24 μM Compound: 4, Nobiletin	Anticancer activity against human HT-29 cells after 72 hrs by MTT assay Anticancer activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 19054677]
LNCaP C4-2	IC₅₀	30.3 μM Compound: 44	Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay	[PMID: 36459083]
MCF7	IC₅₀	4.4 μM Compound: 20	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	4.9 μM Compound: 20	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
Monocyte	IC₅₀	10 μM Compound: Nobiletin	Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA	[PMID: 10096854]
PC-3	IC₅₀	122.6 μM Compound: 44	Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay	[PMID: 36459083]

In Vitro

Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment progressively reduces protein expressions of MMP-2 and MMP-9. In U2OS and HOS cells, Nobiletin considerably reduces the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Nobiletin down-regulates the p-CREB and the SP-1 expressions in the nuclear fraction, whereas Nobiletin does not affect c-Jun and c-Fos expressions^[1].
Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment significantly reduces mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	U2OS and HOS cells
Concentration:	0 μM, 25 μM, 50 μM, 75 μM, 100 μM
Incubation Time:	24 hours
Result:	Progressively reduced protein expressions of MMP-2 and MMP-9. Considerably reduced the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Down-regulated the p-CREB and the SP-1 expressions in the nuclear fraction in U2OS and HOS cells.

RT-PCR^[1]

Cell Line:	U2OS and HOS cells
Concentration:	0 μM, 25 μM, 50 μM, 75 μM, 100 μM
Incubation Time:	24 hours
Result:	Significantly reduced mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells.

In Vivo

Nobiletin (0.1% of regular diet; oral administration; daily; for 20 weeks; male C57BL/6 mice) treatment restores glucose homeostasis and promots energy expenditure and circadian activity in aged mice^[2].

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

Animal Model:	20- to 22-month-old male C57BL/6 mice^[2]
Dosage:	0.1% of regular diet
Administration:	Oral administration; daily; for 20 weeks
Result:	Fully restored glucose tolerance in aged mice, and increased basal body temperature and cold tolerance in aged mice. Led to a twofold increase in distance run/day on voluntary wheels compared with aged regular diet-fed mice during the active phase.

Molecular Weight

402.39

Formula

C₂₁H₂₂O₈

CAS No.

478-01-3

Appearance

Solid

Color

White to off-white

SMILES

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

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (124.26 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	2.4852 mL	12.4258 mL	24.8515 mL
5 mM	0.4970 mL	2.4852 mL	4.9703 mL
10 mM	0.2485 mL	1.2426 mL	2.4852 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.79%

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) HNMR (255 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Cheng HL, et al. Nobiletin inhibits human osteosarcoma cells metastasis by blocking ERK and JNK-mediated MMPs expression. Oncotarget. 2016 Jun 7;7(23):35208-23. [Content Brief]

[2]. Nohara K, et al. Nobiletin fortifies mitochondrial respiration in skeletal muscle to promote healthy aging against metabolic challenge. Nat Commun. 2019 Aug 28;10(1):3923. [Content Brief]

[3]. Takito J, et al. Nerve growth factor enhances the CRE-dependent transcriptional activity activated by nobiletin in PC12 cells. Can J Physiol Pharmacol. 2016 Jul;94(7):728-33. [Content Brief]

[4]. He B, et al. The Small Molecule Nobiletin Targets the Molecular Oscillator to Enhance Circadian Rhythms and Protect against Metabolic Syndrome. Cell Metab. 2016 Apr 12;23(4):610-21. [Content Brief]

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Nobiletin [478-01-3]

Cat# HY-N0155-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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