Biological Information

Background Information:

Helicases are required for genome maintenance and cellular homeostasis. They act as ATP-dependent motor enzymes, unwinding double-stranded DNA-DNA or DNA-RNA duplexes or translocating to single-stranded nucleic acid. Their mutation and/or overexpression are closely associated with many genetic disorders, neurodegenerative diseases, viral infections, tumor development and progression. Cancer cells, to ensure rapid multiplication, need to overuse helicases. These cancer-specific vulnerabilities can thus be exploited to selectively target tumors. WRN (RECQ3) Human Helicase ATPase enzymatic LeadHunter Assay offers a fluorometric assay in HTS and standard format for Hit Finding and hit confirmation. ADP, a universal product of helicase activity, is taken over by several successive enzymes in the ADP Hunter™ Plus assay kit to generate a fluorescent dye. Fluorescent signal is directly proportional to helicase ATPase activity.

Family:

Helicase

Sub Family:

RecQ-like

Class:

ATPase

Protein Name:

WRN

Uniprot Number:

Q14191

Protein Aliases:

DNA helicase, RecQ-like type 3 / RecQ protein-like 2 / Werner syndrome protein

Gene Name:

WRN RecQ like helicase

Gene ID:

7486

Gene Aliases:

WRN, RECQ3, RECQL2, RECQL3

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Detection Method:

Fluorimetry (ADP Hunter ™ Plus)

Testing Information

Substrate:

Deoxyribonucleic acid

Tracer:

ADP

ATP Concentration:

25 µM

Incubation:

60 min at RT

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

10

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5328760

Name

Tyrphostin AG 538

Measurement

1890nM - IC50

PubChem ID

49852229

Name

ML216

Measurement

4700nM - IC50

PubChem ID

166140536

Name

HRO 761

Measurement

110nM - IC50

PubChem ID

170717998

Name

VVD-214

Measurement

10000nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault