APS-2-79 hydrochloride

立即咨询

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。

CAS NO:

2002381-31-7

APS-2-79 hydrochloride 是一种 KSR 依赖性的MEK拮抗剂。APS-2-79 与 ATP^biotin竞争性地结合到 KSR2-MEK1 复合物内的KSR2，IC₅₀为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态，使其无法再结合 RAF 和激活 MEK，从而阻断了 Ras-MAPK 信号通路。

生物活性

APS-2-79 hydrochloride is aKSR-dependentMEKantagonist. APS-2-79 inhibits ATP^biotinbinding to KSR2 within the KSR2-MEK1 complexe with anIC₅₀of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling^[1].

IC₅₀& Target^[1]

KSR2

120 nM (IC₅₀)

MEK1

体外研究
(In Vitro)

APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells^[1].
APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations^[1]

分子量

423.89

Formula

C₂₃H₂₂ClN₃O₃

CAS 号

2002381-31-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.