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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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。 |
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]. |
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]. |
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 |
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 |