EI-52 | ERK-MYD88 inhibitor | Probechem Biochemicals

Chemical Structure : EI-52

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EI-52 (ERK-MYD88 inhibitor)

货号: 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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100 mg		Get quote
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	387.44
分子式	C22H21N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(4-(dimethylamino)phenyl)-N-(6-methoxypyridin-3-yl)-1H-benzo[d]imidazole-5-carboxamide

参考文献

1. Virard F, et al. Nat Commun. 2024 Aug 15;15(1):7037.