Human PDE8A1 (GenBank Accession No. NM_002605), full length with N-terminal GST-tag, MW= 119 kDa, expressed in a Baculovirus infected Sf9 cell expression system.

O60658

PDE8A, phosphodiesterase 8A

≥440 pmol/min/µg.

One unit is defined as the amount of enzyme that will convert 1 pmole of 3', 5'-cAMP to 5'-AMP per minute at 37°C.

Assayed using BPS's PDE8A kit, Cat. # 60380. Assay conditions: 10 mM Tris-HCl, pH 7.4, 10 mM MgCl₂, 0.05% Tween-20, 0.1 mg/ml BSA, 200 µM cAMP, 2.5 kU 5'-nucleotidase, and serial dilutions of PDE8A1 at 37°C for 20 min. Quantified by 5'-nucleotidase cleaving the 5'-AMP product and releasing the phosphate group which is detected by Malachite Green Reagent.

40 mM Tris-HCl, pH 8.0, 110 mM NaCl, 2.2 mM KCl, 3 mM DTT, 0.04% Tween-20 and 20% Glycerol.

Aqueous buffer solution

>6 months at -80°C.

Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.

1. Wu P. and Wang P. Proc. Natl. Acad. Sci. U.S.A. 101 (51), 17634-17639 (2004).
2. Gamanuma M. et al., Cell. Signal. 15 (6), 565-574 (2003).

Application Reference(s):
1. Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders (2017)
2. Utility of Adenosine Monophosphate Detection System for Monitoring the Activities of Diverse Enzyme Reactions (2017)
3. Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders (2017)
4. Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties (2017)
5. Identification and characterization of a potent and biologically-active PDE4/7 inhibitor via fission yeast-based assays (2017)
6. Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity. (2017)
7. Characterization of the binding properties of T-773 as a PET radioligand for phosphodiesterase 10A (2015)
8. Genetic deletion and pharmacological inhibition of phosphodiesterase 10A protects mice from diet-induced obesity and insulin resistance (2014)
9. A yeast-based chemical screen identifies a PDE inhibitor that elevates steroidogenesis in mouse Leydig cells via PDE8 and PDE4 inhibition (2013)
10. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey (2013)

Avoid freeze/thaw cycles.

PDE

Recombinant Protein