ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 μM and enzymatic IC50 values of 0.087 μM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026μM.
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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。 |
描述 | ERK5, encoded by MAPK7 gene, is a member of the MAP kinase family. ERK5 plays a role in various cellular processes such as proliferation, differentiation and cell survival. The upstream activator of ERK5 is the MAPK kinase MAP2K5. Upon activation, ERK5 translocates to the nucleus and phosphorylates various downstream targets. ERK5-IN-1 is an ERK5 selective inhibitor with IC50 of 162nM[2]. At the concentrations of 0.04, 0.2, 1 and 5μM, ERK5-IN-1 concentration-dependently inhibited ERK5 autophosphorylation stimulated by sorbitol in Hela cells. ERK5-IN-1 also inhibited ERK5-mediated AP1 transcriptional activity with an EC50 of 4.2μM, and constitutively active MEK5 co-transfected HEK293 cell system[3]. In mice, the oral bioavailability of ERK5-IN-1 was 90%[2]. |
作用机制 | ERK5-IN-1 target ERK5 in an ATP competitive manner[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.18mL 0.44mL 0.22mL |
10.88mL 2.18mL 1.09mL |
21.76mL 4.35mL 2.18mL |
CAS号 | 1234479-76-5 |
分子式 | C25H29N7O2 |
分子量 | 459.54 |
SMILES Code | O=C1C2=C(C=CC=C2)N(C)C3=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=NC=C3N1C |
MDL No. | MFCD18642659 |
别名 | XMD8-85 |
运输 | 蓝冰 |
InChI Key | DDTPGANIPBKTNU-UHFFFAOYSA-N |
Pubchem ID | 46844147 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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