PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
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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, IC50: 14 nM MEK1, Kd: 99 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。 |
靶点 |
|
描述 | PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.78mL 0.36mL 0.18mL |
8.91mL 1.78mL 0.89mL |
17.82mL 3.56mL 1.78mL |
CAS号 | 391210-00-7 |
分子式 | C16H13BrF3IN2O4 |
分子量 | 561.089 |
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 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(187.14 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |