RU.521

Catalog No.S6841 Batch:S684102

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Technical Data

Formula

C19H12Cl2N4O3
Molecular Weight 415.23 CAS No. 2262452-06-0
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.88 mM)
Ethanol 2 mg/mL (4.81 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2% DMSO 40% PEG 300 5%Tween80 53%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
2%DMSO 98%Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 20 μL of 25 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description RU.521 (RU320521) is an active, potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS) that inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM.
Targets
cGAS/dsDNA complex [1]
(Cell-free assay)		 cGAS [1]
(Cell-free assay)
36.2 nM(Kd) 700 nM
In vitro

RU.521, a cGAS inhibitor, impares the overexpression of interferon-stimulated genes (ISGs) in response to cytolethal distending toxin (CDT), confirming the crucial role of cGAS-STING axis in CDT-induced type I IFN signaling.[2]
In vivo

RU.521 alleviated the inflammatory response and alleviated the damage induced by oxidative stress, leading to cardiac protection via increased Sirt3 expression in the hearts of mice with sepsis.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Mouse Embryonic Fibroblasts (MEFs)

  • Concentrations

    1 μM

  • Incubation Time

    3, 7, 40 days

  • Method

    MEFs are exposed with or without STINGi or cGASi to CDT 7.5 ng/ml for the indicated times or to the H153A CDT mutant for 40 days. The mRNA level of the indicated genes is analyzed by RT-qPCR and the IL-6 or TNFα production in the culture supernatant are determined by ELISA. For ELISA assays, a 2 days exposure to LPS 100 ng/ml is used as positive control.
Animal Study:

[3]
  • Animal Models

    Mice

  • Dosages

    5 mg/kg

  • Administration

    i.p.

Selleck's RU.521 has been cited by 13 publications

ALDH2 deficiency augments atherosclerosis through the USP14-cGAS-dependent polarization of proinflammatory macrophages [ Redox Biol, 2024, 76:103318] PubMed: 39178733
TRPM2-mediated feed-forward loop promotes chondrocyte damage in osteoarthritis via calcium-cGAS-STING-NF-κB pathway [ J Adv Res, 2024, S2090-1232(24)00499-5] PubMed: 39505144
Inhibiting autophagy enhanced mitotic catastrophe-mediated anticancer immune responses by regulating the cGAS-STING pathway [ Cancer Lett, 2024, 586:216695] PubMed: 38325769
Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway [ Virus Res, 2024, 343:199344] PubMed: 38431054
Luteolin inhibits herpes simplex virus 1 infection by activating cyclic guanosine monophosphate-adenosine monophosphate synthase-mediated antiviral innate immunity [ Phytomedicine, 2023, 120:155020] PubMed: 37632997
Spinal TAOK2 contributes to neuropathic pain via cGAS-STING activation in rats [ iScience, 2023, 26(10):107792] PubMed: 37720090
Spinal TAOK2 contributes to neuropathic pain via cGAS-STING activation in rats [ iScience, 2023, 26(10):107792] PubMed: 37720090
FLASH X-ray spares intestinal crypts from pyroptosis initiated by cGAS-STING activation upon radioimmunotherapy [ Proc Natl Acad Sci U S A, 2022, 119(43):e2208506119] PubMed: 36256824
AKT1 Is Required for a Complete Palbociclib-Induced Senescence Phenotype in BRAF-V600E-Driven Human Melanoma [ Cancers (Basel), 2022, 14(3)572] PubMed: 35158840
Inhibition of cGAS in Paraventricular Nucleus Attenuates Hypertensive Heart Injury Via Regulating Microglial Autophagy [ Mol Neurobiol, 2022, 59(11):7006-7024] PubMed: 36070120

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.