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BAY885 {[allProObj[0].p_purity_real_show]}

货号:A1176813

BAY-885 is a highly potent and selective ERK5 inhibitor with IC50 value of 35nM.

BAY885 化学结构 CAS号:2307249-33-6
BAY885 化学结构
CAS号:2307249-33-6
BAY885 3D分子结构
CAS号:2307249-33-6
BAY885 化学结构 CAS号:2307249-33-6
BAY885 3D分子结构 CAS号:2307249-33-6
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BAY885 纯度/质量文件 产品仅供科研

货号:A1176813 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 98+%
FR 180204 +

ERK1, Ki: 0.31 μM

++

ERK2, Ki: 0.14 μM

98%
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。

BAY885 生物活性

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].

BAY885 参考文献

[1]Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. J Med Chem. 2019 Jan 24;62(2):928-940

BAY885 实验方案

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

BAY885 技术信息

CAS号2307249-33-6
分子式C25H28F3N7O2
分子量 515.531
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,Inert atmosphere,Room temperature

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
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