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ERK2/p38α MAPK-IN-1 (Compound 1, In silico Hit-2) is a potent and selective ERK2 and p38α MAPK inhibitor, with an IC50 of 82 μM for ERK2. ERK2/p38α MAPK-IN-1 binds to the allosteric site of ERK2 and p38α MAPK in distinct manners. ERK2/p38α MAPK-IN-1 can be used for the research of type 2 diabetes[1]. | [References]
[1] Hasegawa S, et al. Distinct binding modes of a benzothiazole derivative confer structural bases for increasing ERK2 or p38α MAPK selectivity. Biochem Biophys Res Commun. 2024 Apr 16;704:149707. DOI:10.1016/j.bbrc.2024.149707
[2] Kinoshita T, et al. Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay. Bioorg Med Chem Lett. 2016 Feb 1;26(3):955-958. DOI:10.1016/j.bmcl.2015.12.056 |
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