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516535

GSK2606414

≥99% (HPLC), powder, PERK inhibitor, Calbiochem®

别名:

PERK抑制剂I，GSK2606414

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关于此项目

经验公式（希尔记法）:
C24H20F3N5O
化学文摘社编号:
1337531-89-1
分子量:
451.44
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD25976926
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
200
Storage condition:
OK to freeze, protect from light
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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.

Quality Level

200

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

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

General description

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）。

Biochem/physiol Actions

主靶
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

Packaging

用惰性气体包装

Preparation Note

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。

Other Notes

2024年CiteAb奖——成功的帕金森研究供应商(2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research)

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性：标准处理（A）

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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货号GTIN
516535-5MG04055977198126