RU.521
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Cat.code:
inh-ru521-2
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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).
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.
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 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
C19H12Cl2N4O3
2 mg/ml (4.82 mM) in DMSO
200 ng/ml (482 nM), 20 μg/ml (48.2 μM) for cell culture assays
Negative (tested using EndotoxDetect™ assay)
In vitro cellular assays
Each lot is functionally tested and validated using cellular assays.
CONTENTS
Contents
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Product:RU.521
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Cat code:inh-ru521-2
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Quantity:2 x 2 mg
RU.521 is provided as a translucent film.
Shipping & Storage
- Shipping method: Room temperature
- -20°C
- Avoid repeated freeze-thaw cycles
Storage:
Caution:
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:
DOCUMENTS
Documents
Technical Data Sheet
Validation Data Sheet
Safety Data Sheet
Certificate of analysis
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