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产品名称 | ERK ↓ ↑ | ERK1 ↓ ↑ | ERK2 ↓ ↑ | ERK5 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DEL-22379 |
+
ERK, IC50: 0.5 μM |
+
ERK, IC50: 0.5 μM |
98% | ||||||||||||||||
Pluripotin |
++
ERK1, Kd: 98 nM |
RasGAP | 99%+ | ||||||||||||||||
FR 180204 |
+
ERK1, Ki: 0.31 μM |
++
ERK2, Ki: 0.14 μM |
99%+ | ||||||||||||||||
Ravoxertinib |
+++
ERK1, IC50: 1.1 nM |
++++
ERK2, IC50: 0.3 nM |
99%+ | ||||||||||||||||
SCH772984 |
+++
ERK1, IC50: 4 nM |
++++
ERK2, IC50: 1 nM |
99%+ | ||||||||||||||||
Temuterkib |
+++
ERK1, IC50: 5 nM |
+++
ERK2, IC50: 5 nM |
99%+ | ||||||||||||||||
VX-11e |
+++
ERK2, Ki: <2 nM |
99%+ | |||||||||||||||||
Ulixertinib |
++++
ERK2, IC50: <0.3 nM |
99%+ | |||||||||||||||||
XMD17-109 |
++
ERK5, IC50: 162 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 | The extracellular signal-regulated kinase 5 (ERK5) is a member of the mitogen-activated protein kinase family. It acts as a key regulator of cellular signal transduction and can be activated by environmental stress, mitogens, and cytokines. BAY-885 is a potent and selective ERK5 inhibitor with an IC50 value of 35nM. It inhibited ERK5 transcription in SN12C-MEF2 reporter cell line with an IC50 value of 115nM and an IC90 value of 691nM. BAY-885 did not inhibit the proliferation of cells with ERK5 genomic amplification, including SN12C, SNU-449, and MFM-223 cell lines, or cells with constitutively active ERK5 signaling, such as BT-474 and SKBR-3 cell lines. BAY-885 is highly permeable in the Caco-assay. It exhibited no inhibition on the activity of CYP and hERG up to 20µM and 10µM, respectively. The metabolic stability of BAY-885 is low to moderate in rat hepatocytes and human liver microsomes[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.94mL 0.39mL 0.19mL |
9.70mL 1.94mL 0.97mL |
19.40mL 3.88mL 1.94mL |
CAS号 | 2307249-33-6 |
分子式 | C25H28F3N7O2 |
分子量 | 515.531 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 16 mg/mL(31.04 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 |