HNMT Histamine N-Methyltransferase Human SMMT Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Histamine N-methyltransferase (HNMT) is an S-adenosyl-methionine (AdoMet)-dependent enzyme that catalyses the N-tau-methylation of histamine. The HNMT pathway is the predominant metabolic route in the airway and the only process known to terminate the neurotransmitter actions of histamine in the central nervous system. An HNMT inhibitor will elevate endogenous histamine levels and may augment allergic reactions, but may reduce susceptibility to Alzheimer’s disease, Down’s syndrome and Pick’s disease.
Family:
Epigenetic
Sub Family:
Small Molecule Methyltransferase (SMMT)
Class:
Writer
Protein Name:
Histamine N-Methyltransferase
Uniprot Number:
P50135
Gene Name:
HNMT
Gene ID:
3176
Accession Number:
NM_001024074
Organism:
Human
Construct Details:
Fragment (2-292), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant histamine N-methyltransferase expressed in E. coli-derived is used. Test compound and/or vehicle is preincubated with 0.025 μg/ml enzyme‡ in phosphate buffer pH 7.8 for 15 minutes at 37⁰C. The reaction is initiated by addition of 20 μM histamine, 1.4 µM S-(5'-adenosyl)-L-methionine and 0.014 µM S-adenosyl-L-[methyl-3H]methionine for another 30 minute incubation period and terminated by further addition of 2.5 M borate. The resulting histamine is converted to [3H]N-methylhistamine and separated by column. An aliquot is removed and counted to determine the amount of [3H]N-methylhistamine formed. Compounds are screened at 10 μM.
Substrate:
20 µM Histamine
Incubation:
30 min at 37°C
Control Inhibitor:
Amodiaquine
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
Phenylethanolamine N-Methyltransferase Human Enzymatic LeadHunter Assay - TW
Item: 145700
Questions? Contact Us
You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.
