| 產(chǎn)品描述： | AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM. |
| 靶點(diǎn)： |
ERK5:8 nM (IC50);ERK |
| 體外研究： |
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 |
| 參考文獻(xiàn)： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.541 ml |
7.707 ml |
15.414 ml |
| 5 mM |
0.308 ml |
1.541 ml |
3.083 ml |
| 10 mM |
0.154 ml |
0.771 ml |
1.541 ml |
| 50 mM |
0.031 ml |
0.154 ml |
0.308 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京