516535
GSK2606414
≥99% (HPLC), powder, PERK inhibitor, Calbiochem®
别名:
PERK抑制剂I，GSK2606414
Product Name
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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相关类别
一般描述
一种细胞可透过性的吡咯并嘧啶胺化合物，通过靶向PERK非活性DFG 构象的ATP结合区，发挥高效的EIF2AK3/PERK抑制剂作用 (IC50 = 0.4 nM; [ATP] = 5 µM)。相较对c-Kit、Aurora B、BRK、HRI/EIF2AK1、MLK2/MAP3K10、c-MER、DDR2、PKR/EIF2AK2和MLCK2/MYLK2的作用（IC50分别为 154、407、412、420、452、474、524、696和701 nM），选择性≥385倍。对280多种其它激酶几乎没有活性(IC50 >1 µM)。已证明在A549培养物中配合毒胡萝卜素可体内抑制ER应激-诱导PERK自磷酸化（100%，≤30 nM；60 min预孵育）。并可体内有效抑制小鼠PxBC-3肿瘤生长（50和150 mg/kg/12 h p.o.）。也可以提供25 mM的DMSO溶液（目录号508340）。
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
制备说明
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
免责声明
毒性：标准处理（A）
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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