Biological Information

Background Information:

Janus kinase 2 (JAK2) is a nonreceptor tyrosine kinase belonging to the Janus family. It is activated by a variety of cytokine and growth factor receptors, resulting in signaling cascades that facilitate the activation of various downstream target genes. JAK2 mediates gene transcription through its well-characterized downstream signaling molecules, the signal transducers and activators of transcription proteins (STAT).

Family:

Kinase

Sub Family:

TK

Class:

Protein Tyrosine

Protein Name:

JAK2

Uniprot Number:

O60674

Protein Aliases:

JAK-2

Gene Name:

JAK2

Gene ID:

3717

Gene Aliases:

JTK10

Accession Number:

NM_001322195

Organism:

Human

Construct Details:

Fragment (809-1132), 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 JAK2 expressed in insect cells is used. Test compound and/or vehicle is preincubated with 1.5 µg/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.4. The reaction is initiated by addition of 0.2 mg/ml poly(Glu:Tyr), 10 µM ATP containing 0.25 µCi [γ32P]ATP for 30 minutes and terminated by further addition of 3% H3PO4. An aliquot is counted to determine the radioactivity of [32P]Poly(Glu:Tyr). Compounds are screened at 10 µM.

Substrate:

200 µg/ml Poly(Glu:Tyr)

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:

10

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5328760

Name

Tyrphostin AG 538

Measurement

0.2μM - IC50

PubChem ID

122130844

Name

Staurosporine

Measurement

0.0023μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibition of JAK2 may impair erythropoietin (EPO)-induced erythropoeiesis and protection from bain damage following hypoxia. Inhibition may also adversely effect diabetes.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: 174080