|3-(1-(6,7-二氯-1H-苯并[d]咪唑-2-基)-5-羟基-3-甲基-1H-吡唑-4-基)异苯并呋喃-1(3H)-酮|CsnPharm

CAS No.: 2262452-06-0

RU.521 Catalog No. CSN23556

Synonyms: RU320521;RU-521

RU-521 is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 36.2 nM.

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生物活性

实验方案

技术信息

生物活性

描述Cyclic GMP-AMP synthase (cGAS), acting as a sensor of DNA from pathogens or mislocalized self-DNA, synthesizes a cyclic dinucleotide that initiates an inflammatory cellular response. RU.521 is a potent, small-molecular inhibitor of cGAS. It binds to the cGAS/dsDNA complex with a K_d value of 36.2 nM. In RAW macrophage cells stably expressing an interferon-responsive element coupled to a luciferase gene, RU.521 suppressed dsDNA-activated reporter activity with an IC₅₀ value of 700 nM. When RAW cells were stimulated with immunogenic ligands for RIG-I, Tlr2/1, Tlr3, Tlr4, and JAK/STAT signaling pathways, RU.521 at its EC75 value failed to suppress the activation of cells by all the immunogenic ligands tested. Treatment of BMDM cells isolated from Trex1^−/− mice with RU.521 at its IC₅₀ value for 24 hours significantly decreased IFNB1 expression as compared to DMSO-treated cells^[1].
作用机制RU.521 inhibits cGAS by targeting the pocket of cGAS and subsequently pushing the benzimidazole ring away from the enzyme. It potentially inhibits every catalytic step of cGAS, including substrate binding, intermediate and product formation, or displaces substrates from the catalytic pocket of cGAS.
参考文献

[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. PMID: 28963528; PMCID: PMC5622107.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4083 mL
- 12.0415 mL
- 24.0831 mL
- 5 mM
- 0.4817 mL
- 2.4083 mL
- 4.8166 mL
- 10 mM
- 0.2408 mL
- 1.2042 mL
- 2.4083 mL

技术信息

CAS号

2262452-06-0

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H12Cl2N4O3

运输

蓝冰

分子量

415.23

别名

RU320521;RU-521

溶解度

DMSO	107.5 mg/mL (258.9 mM)
Water	insoluble

动物实验配方

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