Biological Information
Background Information:
Phosphodiesterase 8B (PDE8B) is an enzyme that selectively hydrolyzes cyclic AMP (cAMP), a crucial second messenger involved in various cellular processes. Primarily expressed in the thyroid gland, PDE8B plays a significant role in regulating thyroid hormone signaling by controlling cAMP levels within cells. It is also found in other tissues, including the brain, where it influences neuronal activity. Dysregulation of PDE8B activity has been linked to thyroid disorders and neurological conditions. As a result, PDE8B is being investigated as a potential therapeutic target for diseases related to thyroid dysfunction, neurodegenerative disorders, and other conditions where cAMP signaling is disrupted.
Family:
PDE
Sub Family:
Phosphodiesterase
Class:
Cyclic Nucleotide Signaling
Protein Name:
PDE8B
Uniprot Number:
O95263
Protein Aliases:
Cell proliferation-inducing gene 22 protein
Gene Name:
PDE8B
Gene ID:
8622
Gene Aliases:
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Accession Number:
NM_003719
Organism:
Human
Construct Details:
Fragment (113-End), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Fluorescence Polarization
Measured Response:
Fluorescence Polarization
Testing Information
Procedure Summary:
Human recombinant PDE8B expressed in insect Sf9 cells are used. Test compound and/or vehicle are preincubated with 15.5 ng/ml enzyme in Tris-HCl buffer pH 7.2 for 15 minutes at 25oC. The reaction is initiated by addition of 100 nM fluorescein labeled cAMP and incubated for another 30 minutes. The reaction is terminated by the addition of IMAP binding solution. IMAP complexes with phosphate groups on nucleotide monophosphate generated from cyclic nucleotides through PDE activity are detected. Determination of the amount of complex formed is read spectrofluorimetrically at 470 nm/525 nm. Compounds are screened at 10 µM.
Substrate:
100 nM FAM-cAMP
Incubation:
30 min at 25°C
Control Inhibitor:
Dipyridamole
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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS