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4&mu8C
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
4&mu8C图片
CAS NO:14003-96-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
500mg电议
1g电议

产品介绍
4μ8C (IRE1 Inhibitor III) 是 IRE1α 的小分子抑制剂。
Cas No.14003-96-4
别名4u8C
化学名7-hydroxy-4-methyl-2-oxochromene-8-carbaldehyde
Canonical SMILESCC1=CC(=O)OC2=C1C=CC(=C2C=O)O
分子式C11H8O4
分子量204.18
溶解度≥ 8.65mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

The inositol-requiring enzyme 1α (IRE1α) is a serine-threonine kinase that plays crucial roles in activating the unfolded protein response. Studies suggest that IRE1α is activated during thymic T cell development and in effector CD8+ T cells. 4μ8C is a potent and selective IRE1 Rnase inhibitor.

In vitro: 4μ8c is a potent and non-toxic inhibitor of IRE1 RNase activation in response to both hypoxia and other ER stress-inducing agents. This compound effectively inhibited IRE1 induced activation of the downstream target genes in both HCT116 colorectal cancer and KP4 pancreatic cancer cell lines under hypoxia. However, despite potent inhibition of IRE1 activation and the, 4μ8c had no effect on cell proliferation or clonogenic survival of HCT116 and KP4 cells during exposure to hypoxia or anoxia. Similarly, 4μ8c inhibition of IRE1 did not sensitize cells to other ER stress inducing agents [1].

In vivo: 4μ8C has not been tested in vivo, probably because of its unfavourable pharmacokinetics.

Clinical trial: Up to now, 4μ8C is still in the preclinical development stage.

Reference:
[1] Dan Cojocari, Ravi Vellanki, Brandon Sit, Marianne Koritzinsky, and Bradly G. Wouters. IRE1 and PERK as targets of cellular adaptation and survival to hypoxia. Mol Cancer Ther 2013;12(11 Suppl):C284.
[2] Hetz C, Chevet E, Harding HP. Targeting the unfolded protein response in disease. Nat Rev Drug Discov. 2013 Sep;12(9):703-19.