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製品番号: HY-147129

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cGAS-IN-9

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.

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CAS 番号: 2369750-66-1
分子式: C₁₆H₁₄Cl₂N₄O₂
分子量:365.21

保管条件:

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

cGAS-IN-9 構造式

CAS 番号: 2369750-66-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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製品説明

CXCR アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	2.95 μM Compound: 4; G108	Cytotoxicity against human THP-1 cells assessed as cell growth inhibition Cytotoxicity against human THP-1 cells assessed as cell growth inhibition	[PMID: 34044539]

体外実験

cGAS-IN-9 (Compound G108) (5 h) inhibits dsDNA-induced IFNB1 and CXCL10 mRNA expression in THP1 cells, with IC₅₀ values of 2.95 μM and 3.56 μM, respectively^[1].
cGAS-IN-9 (5 h) inhibits dsDNA-induced IFNB1 and CXCL10 mRNA expression in primary human macrophages, with IC₅₀ values of 1.53 μM and 0.59 μM, respectively^[1].
cGAS-IN-9 (5-10 μM; 5 h) specifically inhibits dsDNA-induced IFNB1 mRNA expression in primary human macrophages at a concentration of 5 μM, while only exhibits weak off-target activity against the cGAMP and hpRNA pathways in THP1 cells at a concentration of 10 μM^[1].
cGAS-IN-9 (25 h) inhibits the activation of cGAS-dependent NF-κB and interferon pathways in THP1-Dual cells, with an IC₅₀ of 2.27 μM for NF-κB reporter gene activity^[1].

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

化学情報

CAS 番号 2369750-66-1
分子量 365.21
分子式 C₁₆H₁₄Cl₂N₄O₂
SMILES

O=C(N1CC=2C=3C(=CC(Cl)=C(Cl)C3NC2CC1)C=4C=NNC4)CO
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Lama L, et al. Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat Commun. 2019;10(1):2261. Published 2019 May 21. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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cGAS-IN-9

CXCR アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

cGAS-IN-9 関連分類

HY-147129 関連分類