产品说明书

AX-15836

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Chemical Structure| 2035509-96-5 同义名 : -
CAS号 : 2035509-96-5
货号 : A798244
分子式 : C32H40N8O5S
纯度 : 99%+
分子量 : 648.776
MDL号 : MFCD30536368
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(161.84 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：
生物活性
描述 AX-15836 is a highly selective inhibitor of ERK5, exhibiting over 1,000-fold selectivity against more than 200 other kinases. It also demonstrates greater selectivity over BRD4, with a Kd of 3,600 nM. AX-15836 shows similar intracellular potency (4–9 nM) across all tested cell types, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and cancer cell lines. It is completely ineffective in inhibiting the inflammatory cytokine response (EC50 > 10 μM), indicating that the BRD inhibition component of the compound mediates the reduction in cytokines. In HUVEC and HeLa cell types, samples treated with AX-15836 exhibit few differentially expressed genes. AX15836 significantly inhibits the phosphorylated form of ERK5 stimulated by EGF in HeLa cells[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.71mL

1.54mL

0.77mL

15.41mL

3.08mL

1.54mL
参考文献

[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.