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![PERK抑制剂I，GSK2606414 GSK2606414 is a cell-permeable, highly potent inhibitor of EIF2AK3/PERK (IC₅₀ = 0.4 nM; [ATP] = 5 µM). Targets PERK in its inactive DFG conformation at the ATP-binding region.](/deepweb/assets/sigmaaldrich/product/structures/180/559/efa716dc-d5fe-4339-a6f0-0103084fc04a/640/efa716dc-d5fe-4339-a6f0-0103084fc04a.png)
产品名称
PKR 抑制剂, The PKR Inhibitor, also referenced under CAS 608512-97-6, controls the biological activity of PKR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
质量水平
方案
≥90% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
orange to orange-brown
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
[s]1c2c(nc1)ccc3c2\C(=C\c4nc[nH]c4)\C(=O)N3
InChI
1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-
InChI key
VFBGXTUGODTSPK-BAQGIRSFSA-N
一般描述
一种咪唑-羟吲哚化合物，作为PKR的一种有效的ATP结合位点定向抑制剂。显示可有效抑制RNA诱导的PKR自磷酸化（IC50 =210 nM）并挽救PKR依赖性翻译阻断（IC50=100 nM）。也可以使用非活性对照（目录号 527455。显示可增加持久突触增强的晚期阶段，并增强小鼠的长期记忆。也可以50 mM的DMSO溶液（货号527451）提供。
一种咪唑-羟吲哚化合物，作为PKR的一种有效的ATP结合位点定向抑制剂。显示可有效抑制RNA诱导的PKR自磷酸化（IC50 =210 nM）并挽救PKR依赖性翻译阻断（IC50=100 nM）。显示可增加持久突触增强的晚期阶段，并增强小鼠的长期记忆。也可以使用非活性对照（目录号527455）。
生化/生理作用
主要靶标
PKR
PKR
产物不与ATP竞争。
可逆：否
细胞渗透性：否
靶标IC50：210 nM抑制RNA诱导的PKR自磷酸化，100 nM挽救PKR依赖性翻译阻断
包装
用惰性气体包装
警告
毒性：致癌/致畸（D）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多3个月。
其他说明
Zhu, P.J., et al. 2011.Cell147, 1384.
Jammi, N.V., et al. 2003.Biochem.Biophys.Res. Commun.308, 50.
Jammi, N.V., et al. 2003.Biochem.Biophys.Res. Commun.308, 50.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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