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说明： Potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS)
别名： RU320521
化学名： 3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]-1(3H)-isobenzofuranone
纯度： ≥98% (HPLC)
生物活性 for RU.521
RU.521 is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor (Kd = 36.2 nM; IC50 values are 0.11 μM and 2.94 μM against m-cGAS and h-cGAS, respectively). RU.521 suppresses dsDNA-activated reporter activity but not 5'ppp-HP20 RNA or murine IFN-β-induced IFN-β1-dependent gene expression. RU.521 reduces constitutive expression of type I interferon in primary macrophages from a mouse model of Aicardi-Goutières syndrome. Pretreatment of chimeric antigen receptor (CAR) redirected T cells with RU.521 increases efficiency of virus-free gene editing by improving cell viability and CAR integration in cell line.
技术数据 for RU.521
| 分子量 | 415.23 |
| 公式 | C19H12Cl2N4O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2262452-06-0 |
| InChI Key | VIQXILLOJLATEF-UHFFFAOYSA-N |
| Smiles | O=C1OC(C=2C=CC=CC12)C3=C(O)N(N=C3C)C4=NC=5C=CC(Cl)=C(Cl)C5N4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for RU.521
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 20.76 | 50 |
制备储备液 for RU.521
以下数据基于产品分子量 415.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.82 mL | 24.08 mL | 48.17 mL |
| 2.5 mM | 0.96 mL | 4.82 mL | 9.63 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.82 mL |
| 25 mM | 0.1 mL | 0.48 mL | 0.96 mL |
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产品说明书 for RU.521
参考文献 for RU.521
参考文献是支持产品生物活性的出版物。
Kath et al (2022) Pharmacological interventions enhance virus-free generation of TRAC-replaced CAR T cells. Mol.Ther.Methods Clin.Dev 25 311 PMID: 35573047
Lama et al (2019) Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat.Commun 10 2261 PMID: 31113940
Vincent et al (2017) Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat.Commun 8 750 PMID: 28963528
Zhou et al (2018) Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell 174 300 PMID: 30007416
Ke et al (2022) cGAS-STING signaling pathway in gastrointestinal inflammatory disease and cancers. FASEB J 36 e22029 PMID: 34907606
Apel et al (2021) The cytosolic DNA sensor cGAS recognizes neutrophil extracellular traps Sci.Signal 14 eaax7942 PMID: 33688080
If you know of a relevant reference for RU.521, please let us know.
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关键词: RU.521, RU.521 supplier, RU521, RU320521, selective, potent, inhibitor, inhibits, cyclic, GMP-AMP, synthase, cGAS, cytosolic, DNA, sensing, cGAS-STING, STING-Dependent, Signaling, Other, Synthases/Synthetases, 7904, Tocris Bioscience
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