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AX-15836
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AX-15836图片
CAS NO:2035509-96-5
规格:98%
分子量:648.78
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
AX-15836是有效,选择性的ERK5抑制剂,IC50值为8nM。
CAS:2035509-96-5
分子式:C32H40N8O5S
分子量:648.78
纯度:98%
存储:Store at -20°C

Background:

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.


AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a Kd of 3,600 nM. AX15836 shows similar intracellular potency (4-9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. AX15836 was completely ineffective (EC50>10 μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells[1].



[1]. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):11865-11870.