Biological Information

Background Information:

Stimulator of interferon genes (STING, or TMEM173) is an endoplasmic reticulum-associated protein that functions as a major regulator of the innate immune response to viral, bacterial infections, highly expressed in hematopoietic cells including T lymphocytes, NK cells, monocytes, myeloid cells as well as various endothelial or epithelial cells and lung, heart, smooth muscle. STING signal pathway is activated by cyclic dinucleotides (CDNs) secreted by intracellular bacteria or 2’3’-cGAMP derived from the intracellular enzyme, cyclic GMP-AMP synthase (cGAS), upon invasion by pathogens and exposure to aberrant self-DNA, which leads to the production of interferons and proinflammatory cytokines. Targeting STING may be a potential for treatment of cancer and modulation of immune responses.

Family:

Immune System

Class:

PRR

Protein Name:

STING_HUMAN

Uniprot Number:

Q86WV6

Gene Name:

STING

Gene ID:

340061

Gene Aliases:

STING, TMEM173

Accession Number:

MF622062.1

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

HEK293T/17

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

Luminescence

Platform:

Plate reader

Measured Response:

Luminescence

Testing Information

Procedure Summary:

HEK293T/17 cells are seeded overnight with reporter and human STING WT transfected mixture. Test compound and/or vehicle is incubated with cells at 37°C, 5% CO₂ for 6 hours. The STING response is evaluated by luciferase assay. Luminescence is measured using a microplate reader. Induction of STING response by 50 percent or more (≥50%) relative to 1 μM diABZI indicates significant response activity. Inhibition of STING response by 50 percent or more (≥50%) relative to 10 nM diABZI indicates significant STING antagonist activity.

Incubation:

360 min at 37°C

Control Activator:

diABZI

Criteria For Significance:

≥ 50% response of diABZI-induced luminescence

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

135564529

Name

2'3'-cGAMP

Measurement

26μM - EC50

PubChem ID

137701219

Name

diABZI

Measurement

0.0046μM - EC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Potential benefit in the treatment of cancer and modulation of immune responses

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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Item: PP316