HIPK2 Human CMGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

Item: 170100

Price: Login to View Pricing

Status: Available

ADD TO CART

OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Homeodomain-interacting protein kinase 2 (HIPK2), a serine/threonine kinase, has been described as a member of a family of nuclear kinases that act as co-repressors for homeodomain transcription factors. HIPK2 can activate p53-mediated transcriptional regulation of MDM2 and antagonize Myc/Ras-induced transformation. HIPK2 may play an important role in the regulation of p53 apoptotic function. Inhibition of HIPK2 may inhibit apoptosis and facilitate tumorigenesis.

Family:

Kinase

Sub Family:

CMGC

Class:

Protein Ser/Thr

Protein Name:

HIPK2

Uniprot Number:

Q9H2X6

Gene Name:

HIPK2

Gene ID:

28996

Accession Number:

NM_022740

Organism:

Human

Construct Details:

Fragment (165-564), 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 HIPK2 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 341 mU/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 50 µg/ml myelin basic protein (MBP), 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]MBP formed. Compounds are screened at 10 µM.

Substrate:

50 µg/ml Myelin basic protein (MBP)

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

1.1μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei