RU.521 (Synonyms: RU-320521) |
Catalog No.GC37570
One-Click Copy Product Info
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RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor that binds to the catalytic domain of cGAS, thereby inhibiting the activation of cGAS by dsDNA. The IC50 value of RU.521 in inhibiting cGAS-mediated signal transduction is 700nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2262452-06-0
Sample solution is provided at 25 µL, 10mM.
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor that binds to the catalytic domain of cGAS, thereby inhibiting the activation of cGAS by dsDNA. The IC50 value of RU.521 in inhibiting cGAS-mediated signal transduction is 700nM[1].
RU.521 (10μM) can inhibit the replication of human metapneumovirus (hMPV) in 16HBE cells, and exogenous addition of interleukin 1 beta (IL-1β) in the presence of RU.521 does not affect hMPV replication (IL-1β can promote hMPV replication) [2]. RU.521 (700nM) can reverse the damage of HUVEC cells caused by neutrophil extracellular traps (NETs) by inhibiting the cGAS/STING pathway[3].
RU.521 (5mg/kg) can inhibit the cGAS-STING pathway and reduce endoplasmic reticulum stress (ERS), thereby alleviating lung injury and promoting pulmonary ventilation function in rats with pulmonary ischemia/reperfusion (I/R)[4]. Intracisternary infusion of RU.521 (0.4mg/kg) in hypertensive mice reduced the expression of cGAS and STING in the paraventricular nucleus (PVN) of mice, and also reduced the LC3II/I ratio and p62 expression level[5].
References:
[1] Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. doi: 10.1038/s41467-017-00833-9. Erratum in: Nat Commun. 2017 Nov 23;8(1):1827.
[2] Wu G, Zhang Y, Niu L, Hu Y, Yang Y, Zhao Y. Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway. Virus Res. 2024 May;343:199344.
[3] Zhang B, Fang Z, Lin Y, et al. RU. 521 protects against neutrophil extracellular traps-induced vascular endothelial injury by inhibiting cGAS/STING pathway[J]. ||| Bangladesh Journal of Pharmacology|||, 2024, 19(2): 59-64.
[4] Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750.
[5] Han C, Qian X, Ren X, Zhang S, Hu L, Li J, Huang Y, Huang R, Ooi K, Lin H, Xia C. Inhibition of cGAS in Paraventricular Nucleus Attenuates Hypertensive Heart Injury Via Regulating Microglial Autophagy. Mol Neurobiol. 2022 Nov;59(11):7006-7024.
| Cell experiment [1]: | |
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Cell lines |
16HBE cells |
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Preparation Method |
16HBE cells were pretreated with 1, 10 and 20μM of the cGAS inhibitor RU.521 for 24h, and then infected with Human metapneumovirus (hMPV) for 48h. |
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Reaction Conditions |
1, 10 and 20μM, 24h |
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Applications |
HMPV replication decreased significantly after 16HBE cells were treated with different concentrations of inhibitors, and 10μM RU.521 had a significant inhibitory effect. |
| Animal experiment [2]: | |
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Animal models |
Lung ischemia/reperfusion（I/R）Sprague-Dawley rats model |
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Preparation Method |
Sprague-Dawley rats were subjected to left hilar occlusion reperfusion surgery to establish a pulmonary I/R model. Rats were intraperitoneally administered with cGAS-specific inhibitor RU.521, STING agonist SR-717, and ERS inhibitor 4-phenylbutyric acid (4-PBA). |
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Dosage form |
5mg/kg, 1h, i.p. |
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Applications |
RU.521 attenuates pulmonary ischemia/reperfusion injury by inhibiting the cGAS-STING pathway. |
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References: [1] Wu G, Zhang Y, Niu L, Hu Y, Yang Y, Zhao Y. Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway. Virus Res. 2024 May;343:199344. [2] Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. |
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| Cas No. | 2262452-06-0 | SDF | |
| Synonyms | RU-320521 | ||
| Canonical SMILES | O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5 | ||
| Formula | C19H12Cl2N4O3 | M.Wt | 415.23 |
| Solubility | DMSO: ≥ 125 mg/mL (301.04 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4083 mL | 12.0415 mL | 24.083 mL |
| 5 mM | 481.7 μL | 2.4083 mL | 4.8166 mL |
| 10 mM | 240.8 μL | 1.2042 mL | 2.4083 mL |
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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 saline, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)