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

PubChem ID

3108

Name

Dipyridamole

Measurement

22μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP168