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Chemical Structure : EI-52
Catalog No.: PC-22946Not For Human Use, Lab Use Only.
EI-52 is a small molecule inhibitor of ERK-MYD88 interaction, binds ERK1/2 (Kd=4.3/2.1 uM), inhibits ERK1/2-MYD88 interaction with IC50 of 3.1/14.7 uM in HTRF assays, induces cancer cell death.
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EI-52 is a small molecule inhibitor of ERK-MYD88 interaction, binds ERK1/2 (Kd=4.3/2.1 uM), inhibits ERK1/2-MYD88 interaction with IC50 of 3.1/14.7 uM in HTRF assays, induces cancer cell death.
EI-52 inhibits endogenous ERK-MYD88 interaction in HCT116 cells.
EI-52 strongly inhibits MYD88 interaction with WT ERK, does not inhibit its interaction with D319N ERK, Asp319 is critical for EI-52 binding to ERK and inhibition of ERK-MYD88 PPI.
EI-52 (8 uM) induced a rapid and robust cancer cell death in human colon cancer cells HCT116 (K-RasG13D).
EI-52 modifies ERK activity and localization, leading to integrated stress response and apoptosis in cancer cells.
EI-52 does not disrupts the cell cycle, without affecting ERK phosphorylation or ERK1/2 kinase activity.
EI-52 induces apoptosis of Lewis lung carcinoma (LLC) cells in vitro (IC50 = 4 μM).
EI-52 (25 or 50 mg/kg, vehicle (PBS, 40% PEG 400, 20% DMSO), i.p.) displays anti-tumor activity in mice and in patient-derived LCC tumor model.
| M.Wt | 387.44 | |
| Formula | C22H21N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Virard F, et al. Nat Commun. 2024 Aug 15;15(1):7037.
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