1. GPCR/G Protein Immunology/Inflammation NF-κB
  2. Guanylate Cyclase Adenylate Cyclase CXCR NF-κB
  3. cGAS-IN-9

cGAS-IN-9 是一种环鸟苷酸-腺苷酸合成酶 (cGAS) 抑制剂,对人源和鼠源的 cGAS 的 IC50 分别为 27.5 nM 和 5.15 μM。cGAS-IN-9 对人可溶性腺苷酸环化酶 (adenylate cyclase) 具有弱抑制作用,其 IC50 为 26.4 μM。cGAS-IN-9 可抑制人源免疫细胞中 dsDNA 诱导的 IFNB1CXCL10 表达,以及 NF-κB 通路的激活。cGAS-IN-9 可用于 cGAS 依赖性炎症疾病的相关研究。

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cGAS-IN-9

cGAS-IN-9 Chemical Structure

CAS No. : 2369750-66-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC50 values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC50 of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases[1].

体外研究
(In Vitro)

cGAS-IN-9 (Compound G108) (5 h) 可抑制 THP1 细胞中由 dsDNA 诱导的 IFNB1 和 CXCL10 mRNA 表达,其 IC50 值分别为 2.95 μM 和 3.56 μM[1]
cGAS-IN-9 (5 h) 可抑制 dsDNA 诱导的原代人巨噬细胞中 IFNB1 和 CXCL10 mRNA 表达,其 IC50 值分别为 1.53 μM 和 0.59 μM[1]
cGAS-IN-9 (5-10 μM; 5h) 可在 5 μM 浓度下特异性抑制原代人巨噬细胞中由 dsDNA 诱导的 IFNB1 mRNA 表达,同时在 10 μM 浓度下对 THP1 细胞中的 cGAMP 和 hpRNA 通路仅表现出微弱的脱靶活性[1]
cGAS-IN-9 (25 h) 可在 THP1-Dual 细胞中抑制 cGAS 依赖性 NF-κB 和干扰素通路的激活,其对 NF-κB 报告基因活性的 IC50 为 2.27 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

365.21

Formula

C16H14Cl2N4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
cGAS-IN-9
目录号:
HY-147129
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