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ERK5-IN-2

产品编号: DC26018 Featured
ERK5-IN-2
结构式
1888305-96-1
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中国地区超过5000个高品质化合物库存
应用领域
ERK5-IN-2 是一种具有口服活性，亚微摩尔效力，选择性的 ERK5 抑制剂，对 ERK5 和 ERK5 MEF2D 的 IC50s 分别是 0.82 μM，3 μM。ERK5-IN-2 不与 BRD4 溴结构域相互作用。ERK5-IN-2 抑制肿瘤异种移植生长和 碱性成纤维细胞生长因子 (bFGF) 驱动的基质胶塞血管的生成。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1888305-96-1
名称:
别名: ERK5-IN 2; ERK5 IN-2; ERK5-IN-2
SMILES: FC1=CC=CC(Br)=C1C(C2=CNC(C(NC3=CC=CN=C3)=O)=C2)=O
分子式: C17H11BrFN3O2
分子量: 388.19
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: ERK5-IN-2 is a novel, potent, orally bioavailable, sub-micromolar, and selective ERK5 inhibitor with selectivity over p38α and BRD4. It has IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis. Extracellular regulated kinase 5 (ERK5) signalling has been implicated in driving a number of cellular phenotypes including endothelial cell angiogenesis and tumour cell motility. Novel ERK5 inhibitors such as ERK5-IN-2 were identified using high throughput screening, with a series of pyrrole-2-carboxamides substituted at the 4-position with an aroyl group being found to exhibit IC50 values in the micromolar range, but having no selectivity against p38α MAP kinase. Truncation of the N-substituent marginally enhanced potency (∼3-fold) against ERK5, but importantly attenuated inhibition of p38α. Systematic variation of the substituents on the aroyl group led to the selective inhibitor 4-(2-bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide (IC50 0.82 μM for ERK5; IC50 > 120 μM for p38α). The crystal structure (PDB 5O7I) of this compound in complex with ERK5 has been solved. This compound was orally bioavailable and inhibited bFGF-driven Matrigel plug angiogenesis and tumour xenograft growth. The selective ERK5 inhibitor described herein provides a lead for further development into a tool compound for more extensive studies seeking to examine the role of ERK5 signalling in cancer and other diseases.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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