RU.521 - Mouse cGAS Inhibitor

InvitroFit™ PRR inhibitor

ABOUT

Specific inhibitor of murine cGAS

RU.521 is described as a small molecule inhibitor of cGAS (cyclic GMP-AMP synthase, cGAMP synthase)[1, 2]. cGAS is the primary sensor of cytosolic double-stranded DNA (dsDNA), a danger signal indicating possible disturbances in homeostasis caused by infection, sterile tissue damage, and/or cancer. cGAS signals through STING and TBK1 to activate the type I interferon (IFN).

More details More details

 

Mode of action:

In a healthy individual, cGAS senses the abnormal presence of cytosolic DNA such as during bacterial or viral infection. In some autoimmune diseases, cGAS can be constitutively activated by mislocalized self-DNA leading to high type I interferon (IFN) production. RU.521 has been demonstrated to reduce IFN production in vitro and ex vivo in models of autoimmune diseases, such as Aicardi-Goutières [1,2].
RU.521 more potently inhibits the activity of murine cGAS compared to human cGAS [2].
 

Key features:

  • Potent inhibitor of murine cGAS
  • InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested.

 

Learn more Read our review on cGAS.

 

References:

1. Vincent J. et al., 2017. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 28(1):750.
2. Zhou W. et al., 2018. Structure of the human cGAS-DNA complex reveals enhanced control of immune surveillance. Cell. 174(2):300-311.

All products are for research use only, and not for human or veterinary use.

InvitroFit™

InvitroFit™ is a high-quality standard specifically adapted for in vitro studies of inhibitors. InvitroFit™ products are highly pure (≥95%) and guaranteed free of bacterial contamination, as confirmed using HEK Blue™ TLR2 and HEK Blue™ TLR4 cellular assays. Each lot is rigorously tested for functional activity using validated (or proprietary) cellular models. This grade ensures reliability and reproducibility for your research applications.

SPECIFICATIONS

Specifications

Chemical formula

C19H12Cl2N4O3

Molecular weight
415.23 g/mol
Purity
≥ 95% (UHPLC)
Solubility

2 mg/ml (4.82 mM) in DMSO

Working concentration

200 ng/ml (482 nM), 20 μg/ml (48.2 μM) for cell culture assays

Endotoxin

Negative (tested using EndotoxDetect™ assay)

Tested applications

In vitro cellular assays

Quality control

Each lot is functionally tested and validated using cellular assays.

CONTENTS

Contents

  • Product: 
    RU.521
  • Cat code: 
    inh-ru521-2
  • Quantity: 
    2 x 2 mg
Notes:

RU.521 is provided as a translucent film.

Shipping & Storage

  • Shipping method:  Room temperature
  • Storage:

    • -20°C
    Stability: The reconstituted product is stable at least 6 months at -20 °C.

    Caution:

    • Avoid repeated freeze-thaw cycles

Details

cGAS

Cyclic GMP-AMP synthase (cGAS, cGAMP synthase) is a critical cytosolic DNA sensor that triggers innate immune responses through the production of type I interferons (IFNs) [1]. In response to cytosolic double‑stranded DNA (dsDNA), cGAS produces the cyclic dinucleotide (CDN) 2’3’-cGAMP.
CDNs bind directly to STING, leading to TBK1‑IRF3-mediated activation of IFN-stimulated response elements (ISRE) in the promoters of IFN-stimulated genes (ISG). The most potent agonist of human STING is 2’3’-cGAMP [2,3].

 

References:

1. Sun L. et al., 2013. Cyclic GMP-AMP synthase is a cytosolic DNA sensor that activates the type I interferon pathway. Science 339(6121):786-91.
2. Gao P. et al., 2013. Cyclic [G(2’,5’)pA(3’,5’)p] is the metazoan second messenger produced by DNA-activated cyclic GMP-AMP synthase. Cell. 153(5):1094-107.
3. Ablasser A. et al., 2013. cGAS produces a 2’-5’-linked cyclic dinucleotide second messenger that activates STING. Nature. 498(7454):380-4.

 

Chemical structure of RU.521:

 

Chemical structure of RU.521

DOCUMENTS

Documents

RU.521

Technical Data Sheet

Safety Data Sheet

Validation Data Sheet

Certificate of analysis

Need a CoA ?

CUSTOMER SERVICE & TECHNICAL SUPPORT

Question about this product ?