Biological Information

Background Information:

Cyclic-AMP exerts its effects in animal cells mainly by activating the enzyme cyclic AMP-dependent protein kinase A (PKA). This enzyme catalyzes transfer of the terminal phosphate group from ATP to specific serines and threonines of selected proteins. Covalent phosphorylation of the appropriate amino acids of specific cellular proteins in turn results in altered cellullar function as a consequence of activation or inactivation of enzymes or altered membrane permeability to ions or other possible effects. PKA is found in all animal cells, and it is known that hormones or transmitters may be mediated by cAMP-stimulated phosphorylation of specific sites on neuronal or non-neuronal cells to exert their physiological function.

Family:

Kinase

Sub Family:

AGC

Class:

Protein Ser/Thr

Protein Name:

PKACalpha

Uniprot Number:

P17612

Gene Name:

PRKACA

Gene ID:

5566

Gene Aliases:

PKACa

Accession Number:

NM_002730

Organism:

Human

Construct Details:

Fragment, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human protein kinase PKA expressed in E. coli. is used. Test compound and/or vehicle is preincubated with 60.7 ng/ml enzyme in modified MOPS buffer pH 7.2 at 37°C for 15 minutes. The reaction is initiated by addition of 0.5 µM PKA substrate peptide, 10 µM ATP and 0.05 µCi [γ-³²P]ATP for another 30 minute incubation period and terminated by further addition of 3 % H₃PO₄. An aliquot is removed to a 96 well multiscreen, washed with H₃PO₄ solution, dried and counted to determine the amount of ³²2P- PKA substrate peptide formed. Compounds are screened at 10 µM.

Substrate:

0.5 µM PKA substrate peptide

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

1-(5-Isoquinolinylsulfonyl)-2-Methylpiperazine

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

3542

Name

1-(5-Isoquinolinylsulfonyl)-2-Methylpiperazine

Measurement

8.7μM - IC50

PubChem ID

122130844

Name

Staurosporine

Measurement

0.011μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei