GLPBio

RU.521

Catalog No.: GC37570Purity:>98.00%Synonyms: RU-320521
COASDSData Sheet
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.

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RU.521
Cas No.: 2262452-06-0
10mM (in 1mL DMSO)In Stock
$77.00
1
1mgIn Stock
$33.00
1
5mgIn Stock
$84.00
1
10mgIn Stock
$147.00
1
25mgIn Stock
$314.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

2 publicationsPublications from researchers using this product

Description

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.

Protocol

Cell experiment [1]:

Cell lines

16HBE cells

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.

Reaction Conditions

1, 10 and 20μM, 24h

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]:

Animal models

Lung ischemia/reperfusion（I/R）Sprague-Dawley rats model

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).

Dosage form

5mg/kg, 1h, i.p.

Applications

RU.521 attenuates pulmonary ischemia/reperfusion injury by inhibiting the cGAS-STING pathway.

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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
2262452-06-0
Synonyms
RU-320521
SMILES
O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5
Molecular Formula
C19H12Cl2N4O3
Molecular Weight
415.23
Solubility
DMSO: ≥ 125 mg/mL (301.04 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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