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ISR activator A8

Chemical Structure : ISR activator A8

CAS No.: 332874-88-1

ISR activator A8 (RIG-I binder)

货号: PC-25644Not For Human Use, Lab Use Only.

ISR activator A8 is a specific small molecule activator of integrated stress response (ISR) through the binding of the cytosolic pattern recognition receptor RIG-I, subsequently activates the heme-regulated inhibitor (HRI) ISR kinase independent of an interferon response.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ISR activator A8 is a specific small molecule activator of integrated stress response (ISR) through the binding of the cytosolic pattern recognition receptor RIG-I, subsequently activates the heme-regulated inhibitor (HRI) ISR kinase independent of an interferon response.
A8 promotes lipid droplet clearance with an EC50 of ~100 to 500 nM across multiple cell lines.
A8 activates an ATF4-firefly luciferase (FLuc) ISR reporter stably expressed in HEK293T cells with EC50 of 10 uM, which could be blocked by ISR inhibitor ISRIB.
A8 induces expression of ISR target genes CHAC1 and CHOP in HEK293T cells and MEF cells.
A8 activates ISR signaling through the noncanonical activation of the HRI kinase.
A8 binds to RIG-I with KD of 0.764 uM in HTRF assays, induces HRI-dependent ISR signaling in HEK293T cells, but independent of interferon signaling associated with RIG-I–dependent MAVS activation.
A8 robustly increases lipid droplet clearance in both MEFWT and MEFA/A cells with an EC50 of ~500 nM.

物理化学性质&存储条件

分子量 451.56
分子式 C23H21N3O3S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

ethyl 2-(2-((3-cyano-4,6-dimethylpyridin-2-yl)thio)acetamido)-4-phenylthiophene-3-carboxylate

参考文献

1. Cuoco CA, et al. Sci Adv. 2025 Oct 31;11(44):eadt3014.

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