PKD2 Human Protein Ser/Thr Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

Item: 171450

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Two serine/threonine protein kinase D isoforms (PKD1 and PKD2), belonging to the polycystin family, are involved in protein-protein and protein-carbohydrate adhesion. The two isoforms are known to interact, and also thought to be ion channel regulators. PKD2 (PKD4, APKD2) bears closest homology with PKCµ and PKCν. Stimuli that activate PKD2 include phorbol esters, gastrin, and classical and novel PKC family members. Defects in PKD (inhibition of function) is responsible for human autosomal dominant polycystic kidney disease (ADPKD) that causes progressive renal failure and may also lead to liver cysts.

Family:

Kinase

Sub Family:

CAMK

Class:

Protein Ser/Thr

Protein Name:

PKD2

Uniprot Number:

Q9BZL6

Protein Aliases:

nPKC-D2

Gene Name:

PRKD2

Gene ID:

25865

Gene Aliases:

PKD2|HSPC187|DKFZP586E0820

Accession Number:

NM_016457

Organism:

Human

Construct Details:

Full Length, 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 protein kinase PKD2 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 100 mU/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 50 µM MAPKAPK, 10 µM ATP and 0.25 µCi [γ32P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]MAPKAPK formed. Compounds are screened at 10 µM.

Substrate:

50 µM MAPKAPK

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

Staurosporine

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

0.0029μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Defects in PKD (inhibition of function) is responsible for human autosomal dominant polycystic kidney disease (ADPKD) that causes progressive renal failure and may also lead to liver cysts.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei