GW284543, also known as UNC10225170, is a 4-anilinoquin(az)oline chemotype that selectively inhibits MEK5.
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产品名称 | MEK ↓ ↑ | MEK1 ↓ ↑ | MEK1/2 ↓ ↑ | MEK2 ↓ ↑ | MEK5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
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Honokiol | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mirdametinib |
++++
MEK, IC50: 0.33 nM |
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Binimetinib |
+++
MEK, IC50: 12 nM |
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BI-847325 |
++
MEK1, IC50: 25 nM |
+++
MEK2, IC50: 4 nM |
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U0126-EtOH |
+
MEK1, IC50: 0.07 μM |
++
MEK2, IC50: 0.06 μM |
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GDC-0623 |
++++
MEK1, IC50: 0.13 nM |
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TAK-733 |
++++
MEK1, IC50: 3.2 nM |
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Trametinib |
++++
MEK1, IC50: 0.92 nM |
++++
MEK2, IC50: 1.8 nM |
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Selumetinib |
+++
MEK1, Kd: 99 nM MEK1, IC50: 14 nM |
+
MEK2, Kd: 530 nM |
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CI-1040 |
++
MEK1, IC50: 17 nM |
++
MEK2, IC50: 17 nM |
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Myricetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Refametinib |
++
MEK1, IC50: 19 nM |
++
MEK2, IC50: 47 nM |
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Cobimetinib |
+++
MEK1, IC50: 4.2 nM |
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PD98059 |
+
MEK1, IC50: 2 μM |
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SL327 |
+
MEK1, IC50: 0.18 μM |
+
MEK2, IC50: 0.22 μM |
AP-1 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
PD318088 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
AZD8330 |
+++
MEK1/2, IC50: 7 nM |
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Pimasertib | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
(E/Z)-BIX02189 |
++++
MEK5, IC50: 1.5 nM |
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(E/Z)-BIX02188 |
+++
MEK5, IC50: 4.3 nM |
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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 | The KRAS gene is an oncogene that encodes a GTPase transductor protein, K-Ras. The mutant KRAS regulates Myc, a transcription factor in MAPK/ERK signaling pathway, via ERK1/2-dependent and independent mechanisms in pancreatic ductal adenocarcinoma. MEK5 is a key component in MAPK pathway that phosphorylates and activates non-classical MAPK ERK5. GW284543, also known as UNC10225170, is a 4-anilinoquin(az)oline chemotype that selectively inhibits MEK5. Treatment of MIA PaCa-2 cells with GW284543 (10 and 20 μM) for 6 h decreased the expression of endogenous Myc protein in a concentration-dependent manner. The GW284543 treatment (10 and 20 μM) also dose-dependently inhibited MEK5 in MIA PaCa-2 cells, as indicated by the reduction in phosphorylated ERK5[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.69mL 0.54mL 0.27mL |
13.43mL 2.69mL 1.34mL |
26.85mL 5.37mL 2.69mL |
CAS号 | 790186-68-4 |
分子式 | C23H20N2O3 |
分子量 | 372.416 |
别名 | UNC10225170 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(322.22 mM),配合低频超声助溶,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 |