RU.521
Based on 86 publication(s) in Google Scholar
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
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- 純度: 99.95%
- CAS 番号: 2262452-06-0
- 分子式: C19H12Cl2N4O3
- 分子量:415.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 RU.521
More- Immunity. 2025 Nov 11;58(11):2670-2684.e10. [Abstract]
- Immunity. 2025 Jul 8;58(7):1670-1687.e12. [Abstract]
- Adv Mater. 2025 Apr;37(17):e2410998. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Nov 20;16(1):10222. [Abstract]
- Nat Commun. 2025 Jan 3;16(1):289. [Abstract]
- Nat Commun. 2023 May 23;14(1):2950. [Abstract]
- Neuron. 2023 Jan 18;111(2):236-255.e7. [Abstract]
- Mol Cell. 2026 Jun 18;86(12):2294-2308.e7. [Abstract]
- Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]
- J Nanobiotechnology. 2025 Nov 25;23(1):737. [Abstract]
- Adv Sci (Weinh). 2024 Jun 18:e2401634. [Abstract]
- Cell Death Dis. 2026 Mar 18;17(1):318. [Abstract]
- Cancer Lett. 2024 Sep 2:217218. [Abstract]
- Int J Biol Sci. 2024 Sep 3;20(12):4713-4730. [Abstract]
- J Immunother Cancer. 2024 Sep 4;12(9):e009318. [Abstract]
- Cell Commun Signal. 2024 Nov 26;22(1):566. [Abstract]
- Cell Commun Signal. 2023 Sep 28;21(1):264. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157493. [Abstract]
- J Hazard Mater. 2024 Jul 10:476:135101. [Abstract]
- Cell Death Discov. 2022 May 11;8(1):258. [Abstract]
- Proc Natl Acad Sci U S A. 2022 Oct 25;119(43):e2207280119. [Abstract]
- Int J Biol Macromol. 2024 Sep 17:135764. [Abstract]
- Neural Regen Res. 2025 Aug 1;20(8):2361-2372. [Abstract]
- EMBO J. 2025 Sep 1. [Abstract]
- Environ Res. 2026 Mar 15:295:123976. [Abstract]
- J Anim Sci Biotechnol. 2025 Dec 29;16(1):181. [Abstract]
- Clin Transl Med. 2025 May;15(5):e70323. [Abstract]
- Cell Rep. 2026 Jun 9;45(6):117515. [Abstract]
- Cell Rep. 2025 Jun 13;44(6):115851. [Abstract]
- Cell Rep. 2025 Jan 30;44(2):115251. [Abstract]
- Cell Rep. 2024 Apr 23;43(4):114088. [Abstract]
- Virulence. 2025 Dec;16(1):2570001. [Abstract]
- CNS Neurosci Ther. 2023 Jul;29(7):2018-2035. [Abstract]
- Biochem Pharmacol. 2025 Sep 14;242(Pt 2):117334. [Abstract]
- Biosensors (Basel). 2026 May 1;16(5):261. [Abstract]
- EMBO Rep. 2023 Dec 6;24(12):e57500. [Abstract]
- Commun Biol. 2025 Dec 17;8(1):1813. [Abstract]
- Commun Biol. 2025 Apr 14;8(1):607. [Abstract]
- Respir Res. 2025 Jun 21;26(1):219. [Abstract]
- Int Immunopharmacol. 2026 Apr 15:175:116411. [Abstract]
- Int Immunopharmacol. 2026 Apr 1:174:116364. [Abstract]
- Int Immunopharmacol. 2025 Oct 22:167:115717. [Abstract]
- Int Immunopharmacol. 2024 Nov 15;143(Pt 3):113591. [Abstract]
- Int Immunopharmacol. 2024 Sep 22;142(Pt B):113171. [Abstract]
- Int Immunopharmacol. 2024 May 10:132:111984. [Abstract]
- Int Immunopharmacol. 2024 Mar 30:130:111641. [Abstract]
- Int Immunopharmacol. 2023 Oct:123:110795. [Abstract]
- Neurochem Int. 2024 Dec 26:105920. [Abstract]
- Neurochem Int. 2024 Jun 4:178:105788. [Abstract]
- mBio. 2021 Oct 26;12(5):e0240821. [Abstract]
- Cancers (Basel). 2023 Sep 7;15(18):4467. [Abstract]
- Exp Neurol. 2023 Jan:359:114269. [Abstract]
- Neuropharmacology. 2025 Mar 19:110426. [Abstract]
- J Cereb Blood Flow Metab. 2023 May;43(5):736-748. [Abstract]
- Neuropharmacology. 2022 Oct 1:217:109206. [Abstract]
- J Inflamm Res. 2025 Apr 21:18:5399-5413. [Abstract]
- Neurochem Res. 2025 Sep 5;50(5):288. [Abstract]
- Neurochem Res. 2024 May 7. [Abstract]
- FASEB J. 2025 Apr 15;39(7):e70530. [Abstract]
- J Virol. 2025 Jun 12:e0069025. [Abstract]
- BMC Cancer. 2024 May 1;24(1):551. [Abstract]
- J Hepatocell Carcinoma. 2025 Mar 19:12:597-614. [Abstract]
- Toxicol Appl Pharmacol. 2025 Aug 9:504:117502. [Abstract]
- Toxicol Appl Pharmacol. 2025 Jan 18:495:117234. [Abstract]
- Appl Biochem Biotechnol. 2025 Feb;197(2):1025-1038. [Abstract]
- Thromb Res. 2026 Apr:260:109663. [Abstract]
- Food Chem Toxicol. 2025 Oct:204:115648. [Abstract]
- Mol Biotechnol. 2025 Jun;67(6):2262-2276. [Abstract]
- Toxicol Lett. 2023 Jan 15:373:62-75. [Abstract]
- Clin Exp Nephrol. 2024 May;28(5):375-390. [Abstract]
- Dev Comp Immunol. 2023 Feb:139:104567. [Abstract]
- Exp Ther Med. 2023 Feb 17;25(4):155. [Abstract]
- In Vitro Cell Dev Biol Anim. 2025 Aug 28. [Abstract]
- Mol Cell Toxicol. 2026 Jan 7.
- Cardiol Res. 2024 Apr;15(2):108-116. [Abstract]
- Res Sq. 2026 Feb 10.
- Res Sq. 2026 Jan 28.
- SSRN. 2026 Jan 10.
- SSRN. 2025 Dec 15.
- Res Sq. 2025 Nov 10.
- Res Sq. 2025 Sep 2.
- J Environ Sci (China). 2025 Dec:158:137-150. [Abstract]
- Res Sq. 2024 May 30.
- Research Square Preprint. 2023 Oct 3.
- Research Square Preprint. 2023 Jul 28.
Customer Validation & Images
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RT-PCR
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WB
生物活性
IC50: 0.7 μM (dsDNA)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H69AR | IC50 |
32.9 μM
Compound: 3; RU-521
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Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
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[PMID: 34044539] |
| THP1-Dual | CC50 |
38.4 μM
Compound: 3; RU-521
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Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
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[PMID: 34044539] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male 8-week-old male mice with LPS injection[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; 5 mg/kg once
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Result:Increased cardiac function and reduced the inflammatory responses, oxidative stress and apoptosis in hearts of mice.
化学情報
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CAS 番号 2262452-06-0
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性状 Solid
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分子量 415.23
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分子式 C19H12Cl2N4O3
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SMILES
O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5
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別名
RU320521
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (86)
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Journal Impact Factor
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Most Recent
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Immunity
Membrane integrity changes upon viral infection activate sphingomyelinase SMPDL3B to restrict cGAS-STING signaling via cGAMP degradation. [Abstract]2025 Nov 11;58(11):2670-2684.e10. PMID: 41175872 -
Immunity
Mitochondrial complex IV remodeling in tumor-associated macrophages amplifies interferon signaling and promotes anti-tumor immunity. [Abstract]2025 Jul 8;58(7):1670-1687.e12. PMID: 40592341 -
Adv Mater
A Polymeric mRNA Vaccine Featuring Enhanced Site-Specific mRNA Delivery and Inherent STING-Stimulating Performance for Tumor Immunotherapy. [Abstract]2025 Apr;37(17):e2410998. PMID: 40095378 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
An inherited mitochondrial DNA mutation remodels inflammatory cytokine responses in macrophages and in vivo in mice. [Abstract]2025 Nov 20;16(1):10222. PMID: 41266309
RU.521 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 20;16(1):10222. [Abstract]
RU.521 (10 μM; 1 h). Ifnb1 expression (LPS 24 h) and interferon-β (IFN-β) release (LPS 6 h) in LPS-stimulated WT and m.5019 A > G macrophages pre-treated with cyclic GMP-AMP synthase (cGAS) inhibitor RU.521 for 1 h (n = 3).
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Nat Commun
Macrophage STING signaling promotes fibrosis in benign airway stenosis via an IL6-STAT3 pathway. [Abstract]2025 Jan 3;16(1):289. PMID: 39753529
RU.521 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 3;16(1):289. [Abstract]
Ru.521 (5 mg/kg, i.p.; 2 h before modeling) administration in mice. H&E staining showing Intratracheal and LP conditions in control and BAS mice at 7th day. Scale bars indicate 200 μm and 50 μm.
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Nat Commun
Gas therapy potentiates aggregation-induced emission luminogen-based photoimmunotherapy of poorly immunogenic tumors through cGAS-STING pathway activation. [Abstract]2023 May 23;14(1):2950. PMID: 37221157 -
Neuron
Driving axon regeneration by orchestrating neuronal and non-neuronal innate immune responses via the IFNγ-cGAS-STING axis. [Abstract]2023 Jan 18;111(2):236-255.e7. PMID: 36370710 -
Mol Cell
2026 Jun 18;86(12):2294-2308.e7. PMID: 42314650 -
Mol Cell
Cytosolic DNA sensing by cGAS/STING promotes TRPV2-mediated Ca2+ release to protect stressed replication forks. [Abstract]2023 Jan 14;S1097-2765(22)01217-5. PMID: 36696898
RU.521 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]
Effects of cGAS inhibition on [Ca2+]i elevation in HeLa cells induced by ssDNA or dsDNA fragment transfection (2 μg/mL, 6 h). RU.521 (20 μM; 4 h before imaging) is added 4 h before imaging.
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J Nanobiotechnology
Ion-interference amplifier nano-system enhances radiotherapy via mitochondrial dysfunction and efferocytosis Inhibition. [Abstract]2025 Nov 25;23(1):737. PMID: 41291692 -
Adv Sci (Weinh)
T Cell-Derived Apoptotic Extracellular Vesicles Hydrolyze cGAMP to Alleviate Radiation Enteritis via Surface Enzyme ENPP1. [Abstract]2024 Jun 18:e2401634. PMID: 38888507 -
Cell Death Dis
Mitochondrial DNA release via VDAC1 in keratinocytes: a key driver of innate immunity and vitiligo pathogenesis. [Abstract]2026 Mar 18;17(1):318. PMID: 41851094 -
Cancer Lett
Loss of Nrf2 aggravates ionizing radiation-induced intestinal injury by activating the cGAS/STING pathway via Pirin. [Abstract]2024 Sep 2:217218. PMID: 39233044 -
Int J Biol Sci
Neutrophil extracellular traps trigger alveolar epithelial cell necroptosis through the cGAS-STING pathway during acute lung injury in mice. [Abstract]2024 Sep 3;20(12):4713-4730. PMID: 39309425 -
J Immunother Cancer
Loss of Annexin A1 in macrophages restrains efferocytosis and remodels immune microenvironment in pancreatic cancer by activating the cGAS/STING pathway. [Abstract]2024 Sep 4;12(9):e009318. PMID: 39237260 -
Cell Commun Signal
Cadmium exposure triggers alveolar epithelial cell pyroptosis by inducing mitochondrial oxidative stress and activating the cGAS-STING pathway. [Abstract]2024 Nov 26;22(1):566. PMID: 39587603
RU.521 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Nov 26;22(1):566. [Abstract]
RU.521 (5 mg/kg; i.p.; daily) in mice. The fluorescence intensity of SFTPC and GSDMD is detected by immunofluorescence (bar = 100 μm).
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Cell Commun Signal
RU.521 mitigates subarachnoid hemorrhage-induced brain injury via regulating microglial polarization and neuroinflammation mediated by the cGAS/STING/NF-κB pathway. [Abstract]2023 Sep 28;21(1):264. PMID: 37770901 -
Phytomedicine
Protocatechuic acid alleviates cGAS-STING-mediated neuroinflammation by enhancing microglial autophagy in mouse models of Parkinson's disease. [Abstract]2025 Nov 25:148:157493. PMID: 41218352 -
J Hazard Mater
GRP78/IRE1 and cGAS/STING pathway crosstalk through CHOP facilitates iodoacetic acid-mediated testosterone decline. [Abstract]2024 Jul 10:476:135101. PMID: 39002476 -
Cell Death Discov
Mitochondrial damage and activation of the cytosolic DNA sensor cGAS-STING pathway lead to cardiac pyroptosis and hypertrophy in diabetic cardiomyopathy mice. [Abstract]2022 May 11;8(1):258. PMID: 35538059 -
Proc Natl Acad Sci U S A
Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]2022 Oct 25;119(43):e2207280119. PMID: 36252040 -
Int J Biol Macromol
2024 Sep 17:135764. PMID: 39299429 -
Neural Regen Res
The cGAS-STING-interferon regulatory factor 7 pathway regulates neuroinflammation in Parkinson's disease. [Abstract]2025 Aug 1;20(8):2361-2372. PMID: 39359093 -
EMBO J
2025 Sep 1. PMID: 40890487 -
Environ Res
Imidacloprid exposure at population-relevant doses induces hepatic lipid dysregulation: Exploring the role of cGAS-STING pathway-mediated hepatocyte senescence. [Abstract]2026 Mar 15:295:123976. PMID: 41653956 -
J Anim Sci Biotechnol
Extracellular vesicles containing microbial DNA contribute to ruminal dysbiosis-induced mastitis by activating cGAS-STING-NF-κB/NLRP3 pathway. [Abstract]2025 Dec 29;16(1):181. PMID: 41466496 -
Clin Transl Med
cGAS/STING signalling in macrophages aggravates obliterative bronchiolitis via an IFN-α-dependent mechanism after orthotopic tracheal transplantation in mice. [Abstract]2025 May;15(5):e70323. PMID: 40292672 -
Cell Rep
2026 Jun 9;45(6):117515. PMID: 42268710 -
Cell Rep
ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. [Abstract]2025 Jun 13;44(6):115851. PMID: 40516055 -
Cell Rep
Exercise-induced adipokine Nrg4 alleviates MASLD by disrupting hepatic cGAS-STING signaling. [Abstract]2025 Jan 30;44(2):115251. PMID: 39891907 -
Cell Rep
IFNα-induced BST2+ tumor-associated macrophages facilitate immunosuppression and tumor growth in pancreatic cancer by ERK-CXCL7 signaling. [Abstract]2024 Apr 23;43(4):114088. PMID: 38602878 -
Virulence
Mycobacterial ESAT-6 triggers cGAS-STING pathway via the GSDMD-NT dependent mitochondria dysfunction. [Abstract]2025 Dec;16(1):2570001. PMID: 41091775 -
CNS Neurosci Ther
Microglial cGAS drives neuroinflammation in the MPTP mouse models of Parkinson's disease. [Abstract]2023 Jul;29(7):2018-2035. PMID: 36914567 -
Biochem Pharmacol
Activation of the Nrf2/HO-1/GPX4 pathway by cGAMP Mitigates oxidative stress and ferroptosis in ischaemic stroke. [Abstract]2025 Sep 14;242(Pt 2):117334. PMID: 40957492 -
Biosensors (Basel)
Imaging Study of MnO2-Based Nanomotors Modulating HIF-1α/Lipid Droplet Biogenesis and Activating the cGAS-STING Pathway. [Abstract]2026 May 1;16(5):261. PMID: 42187457 -
EMBO Rep
2023 Dec 6;24(12):e57500. PMID: 37870259 -
Commun Biol
Microglial RUNX1/RBM47 ablation inhibits neuronal ferroptosis via regulating the cGAS-STING-MEF2C pathway in mice with postoperative cognitive dysfunction. [Abstract]2025 Dec 17;8(1):1813. PMID: 41407921 -
Commun Biol
2025 Apr 14;8(1):607. PMID: 40229503 -
Respir Res
Inhibition of the ATP synthase c subunit ameliorates HDM/LPS-induced inflammatory responses in asthmatic bronchial epithelial cells by blocking the mPTP-mtDNA-cGAS-STING axis. [Abstract]2025 Jun 21;26(1):219. PMID: 40544259 -
Int Immunopharmacol
Targeting VDAC1-dependent mtDNA release attenuates fibroblast innate immune activation and vitiligo pathogenesis. [Abstract]2026 Apr 15:175:116411. PMID: 41722540 -
Int Immunopharmacol
Neuronal TLR4 upregulation activates the cGAS-STING pathway to induce ferroptosis in EAE mice. [Abstract]2026 Apr 1:174:116364. PMID: 41702081 -
Int Immunopharmacol
Mitochondrial DNA contributes to dysbiosis-associated mastitis via activation of the cGAS-STING pathway. [Abstract]2025 Oct 22:167:115717. PMID: 41130091 -
Int Immunopharmacol
2024 Nov 15;143(Pt 3):113591. PMID: 39549546 -
Int Immunopharmacol
Endogenous retroviruses modulate the susceptibility of mice to Staphylococcus aureus-induced mastitis by activating cGAS-STING signaling. [Abstract]2024 Sep 22;142(Pt B):113171. PMID: 39312862 -
Int Immunopharmacol
IGF2 promotes alveolar bone regeneration in murine periodontitis via inhibiting cGAS/STING-mediated M1 macrophage polarization. [Abstract]2024 May 10:132:111984. PMID: 38565043 -
Int Immunopharmacol
Perillaldehyde ameliorates lipopolysaccharide-induced acute lung injury via suppressing the cGAS/STING signaling pathway. [Abstract]2024 Mar 30:130:111641. PMID: 38368770 -
Int Immunopharmacol
IQGAP1 promotes mitochondrial damage and activation of the mtDNA sensor cGAS-STING pathway to induce endothelial cell pyroptosis leading to atherosclerosis. [Abstract]2023 Oct:123:110795. PMID: 37597406 -
Neurochem Int
Ferritinophagy promotes microglia ferroptosis to aggravate neuroinflammation induced by cerebral ischemia-reperfusion injury via activation of the cGAS-STING signaling pathway. [Abstract]2024 Dec 26:105920. PMID: 39732341 -
Neurochem Int
Pharmacological inhibition of cGAS ameliorates postoperative cognitive dysfunction by suppressing caspase-3/GSDME-dependent pyroptosis. [Abstract]2024 Jun 4:178:105788. PMID: 38843953 -
mBio
2021 Oct 26;12(5):e0240821. PMID: 34634939 -
Cancers (Basel)
Increased Response to Immune Checkpoint Inhibitors with Dietary Methionine Restriction in a Colorectal Cancer Model. [Abstract]2023 Sep 7;15(18):4467. PMID: 37760436 -
Exp Neurol
cGAS-STING pathway aggravates early cerebral ischemia-reperfusion injury in mice by activating NCOA4-mediated ferritinophagy. [Abstract]2023 Jan:359:114269. PMID: 36343680 -
Neuropharmacology
Artesunate demonstrates neuroprotective effect through activation of lysosomal function and inhibition of cGAS-STING pathway. [Abstract]2025 Mar 19:110426. PMID: 40118208 -
J Cereb Blood Flow Metab
Activin A alleviates neuronal injury through inhibiting cGAS-STING-mediated autophagy in mice with ischemic stroke. [Abstract]2023 May;43(5):736-748. PMID: 36537048 -
Neuropharmacology
Pharmacological inhibition of the cGAS-STING signaling pathway suppresses microglial M1-polarization in the spinal cord and attenuates neuropathic pain. [Abstract]2022 Oct 1:217:109206. PMID: 35926582 -
J Inflamm Res
Fumarate Hydratase Restrains mtDNA Attenuates LPS-Induced Acute Lung Injury Through cGAS-STING Pathways. [Abstract]2025 Apr 21:18:5399-5413. PMID: 40291460 -
Neurochem Res
Dual Targeting of TLR9 and cGAS-STING Pathways Attenuates Astrocyte Inflammatory Activation: Potential Implication in Multiple Sclerosis. [Abstract]2025 Sep 5;50(5):288. PMID: 40911109 -
Neurochem Res
Regulating NCOA4-Mediated Ferritinophagy for Therapeutic Intervention in Cerebral Ischemia-Reperfusion Injury. [Abstract]2024 May 7. PMID: 38713437 -
FASEB J
2025 Apr 15;39(7):e70530. PMID: 40193045 -
J Virol
African swine fever virus infection enhances CD14-dependent phagocytosis of porcine alveolar macrophages to promote bacterial uptake and apoptotic body-mediated viral transmission. [Abstract]2025 Jun 12:e0069025. PMID: 40503879 -
BMC Cancer
Knockdown of CENPM activates cGAS-STING pathway to inhibit ovarian cancer by promoting pyroptosis. [Abstract]2024 May 1;24(1):551. PMID: 38693472 -
J Hepatocell Carcinoma
Study on the Mechanism of QRICH1 Mediating PRMT1 to Regulate the Arginine Methylation Modification of cGAS to Promote Arsenics-Induced Pyroptosis in Hepatocellular Carcinoma Cells. [Abstract]2025 Mar 19:12:597-614. PMID: 40124968 -
Toxicol Appl Pharmacol
Activation of the cGAS-STING pathway in monocytes exacerbates pulmonary fibrosis induced by paraquat poisoning. [Abstract]2025 Aug 9:504:117502. PMID: 40789441 -
Toxicol Appl Pharmacol
Hesperidin enhanced anti-breast cancer effect and alleviated cisplatin induced nephrotoxicity through silk fibroin delivery system. [Abstract]2025 Jan 18:495:117234. PMID: 39832567 -
Appl Biochem Biotechnol
DKN-01 Suppresses Gastric Cancer Progression Through Activating cGAS-STING Pathway to Block Macrophage M2 Polarization. [Abstract]2025 Feb;197(2):1025-1038. PMID: 39352454 -
Thromb Res
Cold exposure promotes thrombotic risk in ischemic stroke by activating the platelet cGAS-STING pathway. [Abstract]2026 Apr:260:109663. PMID: 41926906 -
Food Chem Toxicol
Mitochondrial DNA leakage and micronucleus formation activate the cGAS-STING pathway in aristolochic acid I-induced nephritis. [Abstract]2025 Oct:204:115648. PMID: 40681081 -
Mol Biotechnol
GNB4 Silencing Promotes Pyroptosis to Inhibit the Development of Glioma by Activating cGAS-STING Pathway. [Abstract]2025 Jun;67(6):2262-2276. PMID: 38814382 -
Toxicol Lett
2023 Jan 15:373:62-75. PMID: 36368621
RU.521 purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2023 Jan 15:373:62-75. [Abstract]
RU.521 (2.4 μM) significantly reduces the elevation of cGAS and STING triggered by ZnONPs in BEAS-2B cells.
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Clin Exp Nephrol
Cytosolic mtDNA-cGAS-STING axis contributes to sepsis-induced acute kidney injury via activating the NLRP3 inflammasome. [Abstract]2024 May;28(5):375-390. PMID: 38238499 -
Dev Comp Immunol
Bovine cyclic GMP-AMP synthase recognizes exogenous double-stranded DNA and activates the STING-depended interferon β production pathway. [Abstract]2023 Feb:139:104567. PMID: 36228808 -
Exp Ther Med
Scutellarin ameliorates ischemia/reperfusion injury‑induced cardiomyocyte apoptosis and cardiac dysfunction via inhibition of the cGAS‑STING pathway. [Abstract]2023 Feb 17;25(4):155. PMID: 36911381 -
In Vitro Cell Dev Biol Anim
Inhibition of cGAS-STING signaling pathway alleviates high glucose-induced mesothelial-mesenchymal transition in human peritoneal mesothelial cell line HMrSV5. [Abstract]2025 Aug 28. PMID: 40877559 -
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Cardiol Res
Increased Cyclic Guanosine Monophosphate and Interleukin-1Beta Is Activated by Mitochondrial Dysfunction and Associated With Heart Failure in Atrial Fibrillation Patients. [Abstract]2024 Apr;15(2):108-116. PMID: 38645829 -
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J Environ Sci (China)
Paternal BDE-209 exposure disrupts spermatogenesis in mouse offspring via cGAS-STING pathway activation and mitophagy inhibition. [Abstract]2025 Dec:158:137-150. PMID: 40841000 -
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溶剤 & 溶解度
DMSO : 83.33 mg/mL (200.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 2 mg/mL (4.82 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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参考文献
[1]. Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. [Content Brief]
[2]. Xu Q, et al. Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice. Life Sci. 2020 Nov 1;260:118315. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4083 mL | 12.0415 mL | 24.0830 mL | 60.2076 mL |
| 5 mM | 0.4817 mL | 2.4083 mL | 4.8166 mL | 12.0415 mL | |
| 10 mM | 0.2408 mL | 1.2042 mL | 2.4083 mL | 6.0208 mL | |
| 15 mM | 0.1606 mL | 0.8028 mL | 1.6055 mL | 4.0138 mL | |
| 20 mM | 0.1204 mL | 0.6021 mL | 1.2042 mL | 3.0104 mL | |
| 25 mM | 0.0963 mL | 0.4817 mL | 0.9633 mL | 2.4083 mL | |
| 30 mM | 0.0803 mL | 0.4014 mL | 0.8028 mL | 2.0069 mL | |
| 40 mM | 0.0602 mL | 0.3010 mL | 0.6021 mL | 1.5052 mL | |
| 50 mM | 0.0482 mL | 0.2408 mL | 0.4817 mL | 1.2042 mL | |
| 60 mM | 0.0401 mL | 0.2007 mL | 0.4014 mL | 1.0035 mL | |
| 80 mM | 0.0301 mL | 0.1505 mL | 0.3010 mL | 0.7526 mL | |
| 100 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6021 mL |
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