Home Immunology & Inflammation cGAS inhibitor PF-06928215 For research use only.

PF-06928215

PF-06928215 is a high affinity inhibitor of cyclic GMP-AMP synthase (cGAS) with an IC50 of 4.9 μM.

PF-06928215 Chemical Structure

PF-06928215 Chemical Structure

CAS: 2378173-15-8

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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Biological Activity

Description PF-06928215 is a high affinity inhibitor of cyclic GMP-AMP synthase (cGAS) with an IC50 of 4.9 μM.
Targets
cGAS [1]
4.9 μM
In vitro
In vitro

PF-06928215, a high affinity inhibitor of Cyclic GMP-AMP synthase (cGAS), has no activity in cellular cGAS assays measuring dsDNA-induced IFN-beta expression via a luciferase reporter. PF-06928215 has minimal effect on cell viability.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research Cell lines THP-1 Dual cells
Concentrations 0.01-100 μM
Incubation Time 1 h
Method

THP-1 Dual cells are pretreated with various concentrations of PF-06928215 (0.01-100 μM) for 1 hr followed by stimulation with salmon sperm DNA for 12 hrs. Media is collected and analyzed for luciferase signal, and cell viability is analyzed.

Chemical Information & Solubility

Molecular Weight 380.40 Formula

C20H20N4O4
CAS No. 2378173-15-8 SDF --
Smiles OC(=O)C1CCCCC1NC(=O)C2=C3N=C(C=C(O)[N]3N=C2)C4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 76 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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