XMD17-109 是一种特异性的ERK-5抑制剂，在 HEK293 细胞系中的EC50为 4.2 μM。

XMD17-109 is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).

在细胞水平,ERK5-IN-1可抑制内皮生长因子诱导的ERK5自磷酸化（EC50：90 nM）。ERK5-IN-1对ERK5的生物化学性质具有有效的抑制作用（IC50：162 nM）。

HeLa cells are maintained in DMEM supplemented with 10% FBS, 2 mM?l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. Before use HeLa cells are serum starved for 16 h in DMEM supplemented with 2 mM?l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. HeLa cells are then incubated with ERK5-IN-1 at the indicated concentrations for 1 h prior to stimulation with 0.5mol/Lsorbitol for 30 min. Cells are lysed in Triton lysis buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 50 mM sodium fluoride, 1 mM sodium pyrophosphate, 0.27mol/Lsucrose, 1 μM microcystin-LR, 1% (v/v) Triton X-100, 0.1% (v/v) 2-mercaptoethanol) and 20 μg of protein loaded per well. Samples are run on 8% polyacrylamide gels using standard methods. Proteins are transferred onto nitrocellulose membranes and specific proteins detected by immunoblotting.

1435488-37-1

C36H46N8O3

638.817

ERK5-IN-1;XMD17 109

DMSO:93 mg/mL (145.6 mM)
Ethanol:93 mg/mL (145.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years