RU.521 (Synonyms: RU-320521) |
| Katalog-Nr.GC37570 |
RU.521 (RU320521) ist ein potenter und selektiver Inhibitor der zyklischen GMP-AMP-Synthase (cGAS) und hemmt die cGAS-vermittelte Hochregulierung von Interferon.
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Cas No.: 2262452-06-0
Sample solution is provided at 25 µL, 10mM.
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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[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.
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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