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XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $79 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $233 | In Stock | |
50 mg | $377 | In Stock | |
100 mg | $567 | In Stock | |
1 mL x 10 mM (in DMSO) | $112 | In Stock |
Description | XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells). |
Targets&IC50 | ERK5:162 nM(EC50) |
In vivo | At the cellular level, ERK5-IN-1 inhibits endothelial growth factor-induced ERK5 autophosphorylation (EC50: 90 nM). It also effectively inhibits the biochemical properties of ERK5 (IC50: 162 nM). |
Cell Research | 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. |
Alias | XMD17 109, ERK5-IN-1 |
Molecular Weight | 638.8 |
Formula | C36H46N8O3 |
Cas No. | 1435488-37-1 |
Smiles | CCOc1cc(ccc1Nc1ncc2N(C)C(=O)c3ccccc3N(C3CCCC3)c2n1)C(=O)N1CCC(CC1)N1CCN(C)CC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (145.6 mM) Ethanol: 93 mg/mL (145.6 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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