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

Melatonin [73-31-4]

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Cat# HY-B0075-1g

Size : 1g

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Description

Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties^[1]^[2]^[3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation^[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress^[5].

IC₅₀ & Target

Microbial Metabolite

Human Endogenous Metabolite

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
AGS	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
BT-549	IC₅₀	30 mM Compound: Melatonin	Antiproliferative activity against human BT549 cells after 24 hrs by MTT assay Antiproliferative activity against human BT549 cells after 24 hrs by MTT assay	[PMID: 29144746]
C6	IC₅₀	> 40 μM Compound: Melatonin	Antiproliferative activity against rat C6 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against rat C6 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34091208]
CHO	EC₅₀	0.026 nM Compound: melatonin	Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader	[PMID: 21568291]
CHO	EC₅₀	0.069 nM Compound: melatonin	Agonist activity at human melatonin receptor-2 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay Agonist activity at human melatonin receptor-2 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay	[PMID: 26023814]
CHO	EC₅₀	0.098 nM Compound: melatonin	Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay	[PMID: 26023814]
CHO	EC₅₀	0.4 nM Compound: MLT	Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr	[PMID: 24417958]
CHO	EC₅₀	0.49 nM Compound: 1	Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1B Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1B	[PMID: 12646022]
CHO	IC₅₀	1.1 x 10^-10 M Compound: Melatonin	Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method	[PMID: 27876250]
CHO	EC₅₀	1.5 nM Compound: Melatonin	Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay	[PMID: 21420861]
CHO	EC₅₀	1.7 nM Compound: MLT	Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr	[PMID: 24417958]
CHO	EC₅₀	2.2 nM Compound: MLT	Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay	[PMID: 20444610]
CHO	EC₅₀	2.24 nM Compound: 1	Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A	[PMID: 12646022]
CHO-K1	IC₅₀	0.21 nM Compound: melatonin	Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs	[PMID: 23403082]
HCT-116	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
HEK293	EC₅₀	1 nM Compound: Melatonin	Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay	[PMID: 31204226]
HEK293	EC₅₀	25 nM Compound: Melatonin	Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay	[PMID: 31204226]
HepG2	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
HepG2	IC₅₀	271 μM Compound: 1, MLT	Antioxidant activity in human HepG2 cells assessed as reduction in H2O2-induced oxidation by DCFH-DA assay Antioxidant activity in human HepG2 cells assessed as reduction in H2O2-induced oxidation by DCFH-DA assay	[PMID: 23332368]
HGC-27	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
MCF7	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
MCF7	IC₅₀	18 mM Compound: Melatonin	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 29144746]
MDA-MB-231	IC₅₀	0.9 μM Compound: Melatonin	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29144746]
MGC-803	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
PC-12	IC₅₀	> 100 μM Compound: MLT	Neuroprotective activity against amyloid beta (25 to 35 amino acid residues) induced damage in rat PC12 cells assessed as cell viability preincubated for 3 hrs followed by addition of amyloid beta (25 to 35 amino acid residues) for 24 hrs by MTT assay Neuroprotective activity against amyloid beta (25 to 35 amino acid residues) induced damage in rat PC12 cells assessed as cell viability preincubated for 3 hrs followed by addition of amyloid beta (25 to 35 amino acid residues) for 24 hrs by MTT assay	[PMID: 26970662]
SGC-7901	IC₅₀	> 30 μM Compound: Melatonin	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33248852]
SH-SY5Y	EC₅₀	> 1 μM Compound: Melatonin	Neuroprotective activity against t-BuOOH-induced oxidative stress in human SH-SY5Y cells assessed as inhibition ROS accumulation pre-incubated for 24 hrs before t-BuOOH challnge for 30 mins by DCFH-DA probe based fluorescence assay Neuroprotective activity against t-BuOOH-induced oxidative stress in human SH-SY5Y cells assessed as inhibition ROS accumulation pre-incubated for 24 hrs before t-BuOOH challnge for 30 mins by DCFH-DA probe based fluorescence assay	[PMID: 29420891]
U-251	IC₅₀	> 40 μM Compound: Melatonin	Antiproliferative activity against human U-251 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human U-251 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34091208]
U-87MG ATCC	IC₅₀	> 40 μM Compound: Melatonin	Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34091208]

In Vivo

Melatonin increases the levels of activated PTEN, RSK-1, mTOR and AMPKα kinases, mildly inhibits ERK-1/2 phosphorylation and Bad phosphorylation, significantly inhibits phosphorylations of S6 Ribosomal Protein, 4E-BP1, GSK-3α and GSK-3β, and slightly increases PRAS40 phosphorylation in animals^[1]. Melatonin ameliorates the neurotoxiciy and astrocyte activation induced by Aβ_1-42 in the cerebral cortex. Melatonin also blocks the reduction in Reelin and Dab1 expression induced by Aβ_1-42^[2]. Melatonin treatment and lack of NLRP3^-/- share similar inhibition of NF-κB and NLRP3 signaling pathway in mice. Melatonin treatment and lack of NLRP3^-/- share some patterns of clock genes expression, and improve cardiomyocytes morphology in mice^[3].

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

Clinical Trial

Molecular Weight

232.28

Formula

C₁₃H₁₆N₂O₂

CAS No.

73-31-4

Appearance

Solid

Color

White to light yellow

SMILES

CC(NCCC1=CNC2=C1C=C(OC)C=C2)=O

Structure Classification

Others

Initial Source

Microorganisms

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 (430.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 12.5 mg/mL (53.81 mM; Need ultrasonic)

H₂O : 1.1 mg/mL (4.74 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.3051 mL	21.5257 mL	43.0515 mL
5 mM	0.8610 mL	4.3051 mL	8.6103 mL
10 mM	0.4305 mL	2.1526 mL	4.3051 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.76 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 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.76 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
Protocol 5

Add each solvent one by one: 2% DMSO 98% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
Protocol 6

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (12.5 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 7

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 EtOH stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 40% PEG300 60% Saline
Solubility: 15 mg/mL (64.58 mM); Clear solution; Need ultrasonic

Purity & Documentation

Purity: 99.93%

Data Sheet (280 KB) SDS (393 KB)

COA (249 KB) HNMR (268 KB) LCMS (95 KB) Elemental Analysis Report (107 KB)

Handling Instructions (2659 KB)

References

[1]. Kilic U, et al. Particular phosphorylation of PI3K/Akt on Thr308 via PDK-1 and PTEN mediates melatonin's neuroprotective activity after focal cerebral ischemia in mice. Redox Biol. 2017 Apr 5;12:657-665 [Content Brief]

[2]. Hu C, et al. Neuroprotective effect of melatonin on soluble Aβ1-42-induced cortical neurodegeneration via Reelin-Dab1 signaling pathway. Neurol Res. 2017 Apr 7:1-1 [Content Brief]

[3]. Rahim I, et al. Melatonin administration to wild-type mice and non-treated NLRP3 mutant mice share similar inhibition of the inflammatory response during sepsis. J Pineal Res. 2017 Mar 31 [Content Brief]

[4]. Bu LJ, et al. Melatonin, a novel selective ATF-6 inhibitor, induces human hepatoma cell apoptosis through COX-2 downregulation. World J Gastroenterol. 2017 Feb 14;23(6):986-998. [Content Brief]

[5]. Zhi Chen, et al. Melatonin attenuates palmitic acid-induced mouse granulosa cells apoptosis via endoplasmic reticulum stress. J Ovarian Res. 2019 May 10;12(1):43. [Content Brief]

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