Home GPCR & G Protein MT Receptor agonist - ATF/CREB & c-Fos/c-Jun inhibitor - COX inhibitor - Autophagy modulator - Apoptosis related modulator - Mitophagy activator Melatonin For research use only.

Melatonin

Synonyms: NSC 56423, N-Acetyl-5-methoxytryptamine,NSC 113928,MT

Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.

Melatonin Chemical Structure

Melatonin Chemical Structure

CAS No. 73-31-4

Purity & Quality Control

Melatonin Related Products

Signaling Pathway

MT Receptor Signaling Pathways

MT Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=0.00008μM 9435890
CHO Function assay Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1B expressed in CHO cells, Ki=0.00012μM 9435890
NIH3T3 Function assay Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells, Ki=0.0002951μM 9733487
NIH 3T3 Function assay Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00033μM 10737738
NIH 3T3 Function assay Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00066μM 10737738
HEK293 Function assay Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.0002μM 11063602
HEK293 Function assay Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.00053μM 11063602
NIH 3T3 Function assay Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin, Ki=0.0002818μM 11520198
NIH 3T3 Function assay Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand, Ki=0.0002884μM 11520198
HEK293 Function assay Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells, Ki=0.00012μM 11960497
HEK293 Function assay Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells, Ki=0.00031μM 11960497
HEK293 Function assay Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand., Ki=0.00031μM 12061881
CHO Function assay Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells, EC50=0.00047μM 12061881
CHO Function assay Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A, EC50=0.00192μM 12061881
CHO Function assay Ability to inhibit 2-[125I]iodomelatonin specific binding to human melatonin receptor type 1A (MT1) expressed in CHO cells., Ki=0.0000823μM 12213062
CHO Function assay Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells, Ki=0.0000823μM 12213063
HEK293 Function assay Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00014μM 12646022
HEK293 Function assay Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00041μM 12646022
NIH3T3 Function assay Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells, Ki=0.0003μM 14643330
NIH3T3 Function assay Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells., Ki=0.0004μM 14643330
NIH3T3 Function assay Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0003μM 14980664
NIH3T3 Function assay Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0004μM 14980664
NIH3T3 Function assay Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells, Ki=0.0002818μM 15293992
NIH3T3 Function assay Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells, Ki=0.0002884μM 15293992
NIH3T3 Function assay Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0003μM 15380218
NIH3T3 Function assay Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0007μM 15380218
NIH3T3 Function assay Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0003μM 15713384
NIH3T3 Function assay Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0007μM 15713384
NIH3T3 Function assay Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells , Ki=0.0002818μM 15943478
NIH3T3 Function assay Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells, Ki=0.0002884μM 15943478
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.00035μM 16759094
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.00039μM 16759094
NIH3T3 Function assay 1 nM Activity at MT1 receptor expressed in NIH3T3 cells assessed as inhibition of forskolin-stimulated cAMP synthesis at 1 nM 16759094
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells, Ki=0.000257μM 17149869
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells, Ki=0.0003236μM 17149869
NIH 3T3 Function assay Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells, Ki=0.0003548μM 17346859
NIH 3T3 Function assay Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells, Ki=0.000389μM 17346859
NIH3T3 Function assay Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.000263μM 17459711
NIH3T3 Function assay Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.0003388μM 17459711
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0002μM 17481904
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0003μM 17481904
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0001413μM 18052314
NIH3T3 Function assay Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0002399μM 18052314
HEK293 Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, IC50=0.0002μM 18372181
HEK293 Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells, IC50=0.00053μM 18372181
CHO Function assay Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells, IC50=0.06457μM 18400335
CHO Function assay Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells, Ki=0.000525μM 18657980
CHO Function assay Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells, Ki=0.000741μM 18657980
HEK293 Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM 18778943
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00041μM 18778943
CHO Function assay Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay, EC50=0.00049μM 18778943
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM 19193160
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM 19193160
CHO Function assay Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00049μM 19329323
CHO Function assay Agonist activity at human MT1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00224μM 19329323
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting, Ki=0.0004571μM 19473848
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting, Ki=0.000955μM 19473848
CHO Function assay 60 mins Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000296μM 20227878
CHO Function assay 60 mins Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000429μM 20227878
CHO Function assay Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00049μM 20444610
CHO Function assay Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0022μM 20444610
NIH3T3 Function assay 90 mins Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003311μM 20674373
NIH3T3 Function assay 90 mins Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0006166μM 20674373
CHO-Galpha16 Function assay 20 mins Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.00056μM 21237644
CHO-Galpha16 Function assay Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells, Ki=0.00058μM 21237644
CHO-Galpha16 Function assay Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells, Ki=0.00099μM 21237644
CHO-Galpha16 Function assay 20 mins Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.0011μM 21237644
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00022μM 21392858
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00035μM 21392858
HEK293 Function assay Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00025μM 21420861
HEK293 Function assay Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00034μM 21420861
CHO Function assay Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00042μM 21420861
CHO Function assay Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0015μM 21420861
CHO Function assay 30 mins Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0000257μM 21473625
CHO Function assay Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting, Ki=0.00021μM 21473625
CHO Function assay Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting, Ki=0.00024μM 21473625
CHO Function assay 30 mins Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0008511μM 21473625
CHO Function assay 30 mins 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, EC50=0.000026μM 21568291
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00021μM 21568291
CHO Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00024μM 21568291
CHO Function assay 30 mins Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.00082μM 21568291
HEK293 Function assay Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00025μM 21764185
HEK293 Function assay Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00034μM 21764185
NIH3T3 Function assay 90 mins Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.000263μM 22047556
NIH3T3 Function assay 90 mins Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003388μM 22047556
CHO Function assay 60 mins Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000296μM 23228808
CHO Function assay 60 mins Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000429μM 23228808
HEK293 Function assay 2 hrs Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0002μM 23265885
HEK293 Function assay 2 hrs Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0005μM 23265885
CHOK1 Function assay 3 hrs Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, Ki=0.00011μM 23403082
CHOK1 Function assay 3 hrs Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.00021μM 23403082
CHO Function assay 1 hr Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0004μM 24417958
CHO Function assay 1 hr Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0017μM 24417958
Primary neural stem cells Neurogenic assay 10 uM 48 hrs Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring TuJ1 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry 24738476
Primary neural stem cells Neurogenic assay 10 uM 48 hrs Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring MAP-2 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry 24738476
HEK293 Function assay Displacement of [125L]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM 24930835
HEK293 Function assay Displacement of [125L]iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00041μM 24930835
HEK293 Function assay 120 mins Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00014μM 25232966
HEK293 Function assay 120 mins Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00041μM 25232966
SH-SY5Y Neuroprotective assay 10 uM 24 hrs Neuroprotective activity against H2O2-induced oxidative stress-associated death in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 24 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay 26363866
HEK293 Function assay 120 mins Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00025μM 26785296
HEK293 Function assay 120 mins Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00034μM 26785296
CHO Function assay Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells, IC50=0.00011μM 26988801
PC12 Neuroprotective assay 10 uM 2 hrs Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay 27460699
PC12 Neuroprotective assay 20 uM 24 hrs Neuroprotective activity against amyloid beta (1 to 42 residues) induced cell death in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 24 hrs followed by amyloid beta (1 to 42 residues) addition measured after 24 hrs by MTT 27484514
CHO Function assay 60 mins Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method, IC50=0.00011μM 27876250
PC12 Neuroprotective assay 25 uM 2 hrs Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay 28800459
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.9μM 29144746
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
HEK293 Function assay Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.001μM 31204226
HEK293 Function assay Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.025μM 31204226
COS7 Function assay 1.5 hrs Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00018μM 31727472
NIH3T3 Function assay 90 mins Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.0002042μM 31727472
NIH3T3 Function assay 90 mins Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.000302μM 31727472
NIH3T3 Function assay Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00033μM 31727472
CHO Function assay 1 hr Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00046μM 31727472
NIH3T3 Function assay Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00066μM 31727472
COS7 Function assay 1.5 hrs Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00088μM 31727472
CHO Function assay 1 hr Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00095μM 31727472
CHO Function assay Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00013μM ChEMBL
CHO Function assay Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells, Ki=0.0002μM ChEMBL
CHO Function assay Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00023μM ChEMBL
CHO Function assay Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells, Ki=0.00029μM ChEMBL
CHO Function assay Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM ChEMBL
CHO Function assay Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells by Gamma counting, Ki=0.0004571μM ChEMBL
CHO Function assay 1 hr Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.0004571μM ChEMBL
CHO Function assay Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM ChEMBL
CHO Function assay Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells by Gamma counting, Ki=0.000955μM ChEMBL
CHO Function assay 1 hr Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.000955μM ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Targets
melatonin receptor [1]
In vitro
In vitro

Melatonin interacts with the highly toxic hydroxyl radical with a rate constant equivalent to that of other highly efficient hydroxyl radical scavengers. Melatonin reportedly neutralizes hydrogen peroxide, singlet oxygen, peroxynitrite anion, nitric oxide and hypochlorous acid. [1]

Melatonin is believed to scavenge the highly toxic hydroxyl radical, the peroxynitrite anion, and possibly the peroxyl radical. Melatonin reportedly scavenges the superoxide anion radical and it quenches singlet oxygen. Melatonin stimulates mRNA levels for superoxide dismutase and the activities of glutathione peroxidase, glutathione reductase and glucose-6-phosphate dehydrogenase (all of which are antioxidative enzymes), thereby increasing its antioxidative capacity. [2]

Melatonin in cell-free systems has been shown to directly scavenge H2O2, singlet oxygen (1O2) and nitric oxide (NO*), with little or no ability to scavenge the superoxide anion radical (O2*-) in vitro. Melatonin also directly detoxifies the peroxynitrite anion (ONOO-) and/or peroxynitrous acid (ONOOH), or the activated form of this molecule, ONOOH*. Melatonin acts as a direct free radical scavenger with the ability to detoxify both reactive oxygen and reactive nitrogen species. [3]

Melatonin inhibits cAMP accumulation in most of the cells examined, but the indole effects on other messengers have been often observed only in one type of the cells or tissue, until now. Melatonin also regulates the transcription factors, namely, phosphorylation of cAMP-responsive element binding protein and expression of c-Fos. [4]
Cell Research Cell lines HepG2 cells
Concentrations 1.2 mM
Incubation Time 24 h
Method

Cells were treated with various concentrations of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot MT1 / MT2 / p-CREB / CREB / BDNF p-Raf / p-ERK / p-p90RSK / PKAα / p-AKT / p-JNK / p-CaMKII 29570621
In Vivo
In vivo

Melatonin ameliorates necrotizing enterocolitis by preventing Th17/Treg imbalance through activation of the AMPK/SIRT1 pathway
Animal Research Animal Models C57BL/6 mice
Dosages 10 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04521972 Not yet recruiting
Pregnancy Related|Labor; Poor|Uterine Contractions Weak
Michigan State University|McLaren Health Care
 October 1 2024 Not Applicable
NCT06390267 Not yet recruiting
Acute Stress Reaction|Cognitive Performance
Spark Biomedical Inc.|Battelle Memorial Institute
 August 2024 Not Applicable
NCT06343805 Not yet recruiting
Primary Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|PMF|PPV-MF|PET-MF
Ajax Therapeutics Inc.
 July 15 2024 Phase 1

Chemical Information & Solubility

Molecular Weight 232.28 Formula

C13H16N2O2
CAS No. 73-31-4 SDF Download Melatonin SDF
Smiles CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (198.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


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