DRAK1 Human CAMK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

Item: 175590

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Protein serine/threonine kinases DRAK1 and DRAK2 (Death Receptor Associated Kinase 1 and 2) have high sequence homology to DAP (Death-associated protein kinase) and ZIP kinases; both DRACKs are exclusively localized to the cell nucleus. Their kinase domains are involved in the apoptotic signaling induced by interferon-γ.

Family:

Kinase

Sub Family:

CAMK

Class:

Protein Ser/Thr

Protein Name:

DRAK1

Uniprot Number:

Q9UEE5

Protein Aliases:

death-associated protein kinase-related 1

Gene Name:

STK17A

Gene ID:

9263

Gene Aliases:

DRAK1

Accession Number:

NM_004760

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 DRAK1 expressed in insect cells is used. Test compound and/or vehicle is preincubated with 1 μg/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 50 μM ZIPtide , 10 μM ATP and 0.25 μCi [γ32P]ATP for another 30 minutes incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]ZIPtide formed. Compounds are screened at 10 μM.

Substrate:

50 µM ZIPtide

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

0.013μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Kinase DRAK1 inhibitors may inhibit apoptosis and thereby facilitate tumor growth.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei