推荐产品
产品名称
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.
质量水平
方案
≥99% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
O=C(CC1=CC=CC(C(F)(F)F)=C1)N2CCC3=C2C=CC(C4=CN(C)C5=C4C(N)=NC=N5)=C3
InChI
1S/C24H19F4N5O/c1-32-11-18(21-22(29)30-12-31-23(21)32)14-2-3-19-15(9-14)4-5-33(19)20(34)8-13-6-16(24(26,27)28)10-17(25)7-13/h2-3,6-7,9-12H,4-5,8H2,1H3,(H2,29,30,31)
InChI key
PXVQGBJMIQCDEX-UHFFFAOYSA-N
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一般描述
一种细胞可透过性的吡咯并嘧啶胺化合物，通过将 PERK 的非活性DFG 构象靶向 ATP 结合区，从而可作为高效的 EIF2AK3/PERK 抑制剂（IC50 = 0.4 nM；[ATP] = 5 µM），并且表现出比对 c-Kit、Aurora B、BRK、HRI/EIF2AK1、MLK2/MAP3K10、c-MER、DDR2、PKR/EIF2AK2 和 MLCK2/MYLK2 的选择性 ≥385 倍（IC50 分别为 154、407、412、420、452、474、524、696 和 701 nM），对超过 280 种其他激酶的几乎没有活性（IC50 >1 µM）。研究表明，可阻断在 A549 培养物中添加毒胡萝卜素（货号 586005）后的 ER 应激诱导的 PERK 自磷酸化（在体外）（100％，浓度为 30 ≤nM；预孵育 60 分钟），并在体内有效阻滞 PxBC-3 肿瘤的生长（50 和 150 mg/kg/12 h，口服给药）。还可以提供在DMSO（货号508340）中的25 mM溶液。
生化/生理作用
主靶
Perk
Perk
可逆性：是
细胞可渗透性：具有
靶标IC50：针对 EIF2AK3/PERK 催化的 EIF2&α 的值为 0.4 nM
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
溶解后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多6个月。
其他说明
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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