1. Cell Cycle/DNA Damage
  2. Eukaryotic Initiation Factor (eIF)
  3. ISR activator 2

ISR activator 2 是一种选择性 ISR 激活剂。ISR activator 2 可通过与胞质模式识别受体 RIG-I 结合而优先激活 ISR,随后 RIG-I 可激活血红素调节抑制剂 (HRI) ISR 激酶,且该过程不依赖于干扰素反应。ISR activator 2 可用于胰腺癌的研究。

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ISR activator 2

ISR activator 2 Chemical Structure

CAS No. : 332874-88-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ISR activator 2 is a selective ISR activator. ISR activator 2 can preferentially activate the ISR through the binding of the cytosolic pattern recognition receptor RIG-I, which subsequently activates the heme-regulated inhibitor (HRI) ISR kinase independent of an interferon response. ISR activator 2 can be used for the study of pancreatic cancer[1].

体外研究
(In Vitro)

ISR activator 2 (Compound A8) (10 μM,8 小时) 可诱导 HEK293T 细胞中 UPR (未折叠蛋白反应) 和 mTORC1 信号通路基因集的富集。进一步分析表明,这种富集是由于 ISR 靶基因 (如 ASNS、DDIT4、CHAC1 和 CHOP) 表达增加所致[1]
ISR activator 2 (16 小时) 以浓度依赖的方式激活稳定表达 ATF4-FLuc 报告基因的 HEK293T 细胞中的 ATF4-FLuc 报告基因 (EC50 = 10.53 μM) ,并且这种激活可被 ISR 抑制剂 ISRIB (200 nM) 阻断[1]
ISR activator 2 (10 μM,16 小时) 可激活稳定表达 ATF4-mAPPLE 报告基因的 HEK293T 细胞中的 ATF4-mAPPLE 报告基因,但 HRI 敲低完全阻断了这种激活,而 PERK、GCN2 或 PKR 敲低则无影响[1]
ISR activator 2 (0.625-5 μM) 浓度依赖性地抑制 RIG-I 与 dsRNA 探针的结合 (KD = 0.764 μM)[1]
RIG-I 敲低可阻断 ISR activator 2 (10 μM,4 小时) 诱导的 CHAC1 和 CHOP 表达增加[1]
ISR activator 2 (20 小时) 浓度依赖性地促进 MEFWT 细胞中脂滴的清除,并且在 ISR 缺陷细胞 (MEFA/A) 中仍然有效[1]
ISR activator 2 (10 μM, 4 h) 通过其代谢物 CC81 在 HEK293T 和 SW1990 细胞中表现出可分离的 ISR 激活和脂滴清除活性[1]

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

Real Time qPCR[1]

Cell Line: HEK293T cells transfected with nonsilencing or RIGI siRNA
Concentration: 10 μM
Incubation Time: 4 h
Result: RIGI knockdown blocked the increase in CHAC1 and CHOP expression.
分子量

451.56

Formula

C23H21N3O3S2

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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ISR activator 2
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HY-179524
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