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PD 198306 {[allProObj[0].p_purity_real_show]}

货号:A1209818

PD 198306是一种选择性 MAPK/ERK 激酶 (MEK) 抑制剂,能够显著降低Streptozocin诱导的ERK1/2活性升高,具有抗痛觉过敏作用,并可用于与MAPK/ERK相关疾病的研究。

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PD 198306 化学结构 CAS号:212631-61-3
PD 198306 化学结构
CAS号:212631-61-3
PD 198306 3D分子结构
CAS号:212631-61-3
PD 198306 化学结构 CAS号:212631-61-3
PD 198306 3D分子结构 CAS号:212631-61-3
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PD 198306 纯度/质量文件 产品仅供科研

货号:A1209818 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MEK MEK1 MEK1/2 MEK2 MEK5 其他靶点 纯度
Honokiol 98%
Mirdametinib ++++

MEK, IC50: 0.33 nM

99%+
Binimetinib +++

MEK, IC50: 12 nM

99%+
BI-847325 ++

MEK1, IC50: 25 nM

+++

MEK2, IC50: 4 nM

99%+
U0126-EtOH +

MEK1, IC50: 0.07 μM

++

MEK2, IC50: 0.06 μM

98%
GDC-0623 ++++

MEK1, IC50: 0.13 nM

99%+
TAK-733 ++++

MEK1, IC50: 3.2 nM

99%+
Trametinib ++++

MEK1, IC50: 0.92 nM

++++

MEK2, IC50: 1.8 nM

99%+
Selumetinib +++

MEK1, Kd: 99 nM

MEK1, IC50: 14 nM

+

MEK2, Kd: 530 nM

99%+
CI-1040 ++

MEK1, IC50: 17 nM

++

MEK2, IC50: 17 nM

99%+
Myricetin 98%
Refametinib ++

MEK1, IC50: 19 nM

++

MEK2, IC50: 47 nM

99%+
Cobimetinib +++

MEK1, IC50: 4.2 nM

99%+
PD98059 +

MEK1, IC50: 2 μM

99%+
SL327 +

MEK1, IC50: 0.18 μM

+

MEK2, IC50: 0.22 μM

AP-1 98+%
PD318088 98%
AZD8330 +++

MEK1/2, IC50: 7 nM

99%+
Pimasertib 98%
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

99%+
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

PD 198306 生物活性

描述 PD 198306 is a selective MAPK/ERK kinase inhibitor, which significantly reduces the Streptozocin-induced increase in active ERK1 and 2 levels[1].At a concentration of 10 μM for 36 hours, PD 198306 significantly inhibited Tha-GFP replication by 25%[2].In iPSC cells, at a concentration of 5 μM, PD 198306 significantly reduced Tha-Crimson replication by 20% within 18 hours, but this result could not be confirmed at 36 hours[2].

PD 198306 动物研究

Animal study Administered using intrathecal injection (1-30 μg per 10 μL), PD 198306 dose-dependently (1-30 μg) blocked static allodynia both in streptozotocin and in chronic constriction injury (CCI) rat models of neuropathic pain[1].

PD 198306 参考文献

[1]A Ciruela, et al. Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br J Pharmacol. 2003 Mar;138(5):751-6.

[2]Benoit Besson, et al. Kinome-Wide RNA Interference Screening Identifies Mitogen-Activated Protein Kinases and Phosphatidylinositol Metabolism as Key Factors for Rabies Virus Infection. mSphere. 2019 May 22;4(3):e00047-19.

PD 198306 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.50mL

2.10mL

1.05mL

21.00mL

4.20mL

2.10mL

PD 198306 技术信息

CAS号212631-61-3
分子式C18H16F3IN2O2
分子量 476.231
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度
动物实验配方
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