AX-15836

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、高选择性的 ERK5 抑制剂，IC50 为 8 nM；对 BRD4 的亲和力很小（Kd=3.6 uM）。

A potent, highly selective ERK5 inhibitor with IC50 of 8 nM; shows little affinity for BRD4 (Kd=3.6 uM); clearly inhibits the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells.

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.

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AX15836

MAPK/ERK Signaling

ERK

ERK

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2035509-96-5

648.783

C32H40N8O5S

>98% (HPLC)

DMSO : ≥ 101 mg/mL 155.68 mM

O=C1C2=CC=CC=C2N(S(=O)(C)=O)C3=NC(NC4=CC=C(C(N5CCC(N6CCN(C)CC6)CC5)=O)C=C4OCC)=NC=C3N1C

6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-11-(methylsulfonyl)-

(-20℃)

With Ice Pack

≥ 2 years