MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of SIK substrate CRTC3 at S370. MRT199665 induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells.

MRT199665 also causes a decrease in total MEF2C protein. MRT199665 (1 μM; pre-treated for 1 h) enhances LPS (100 ng/mL; stimulated for up to 24 h)-stimulated IL-10 mRNA and Nurr77 mRNA production, and IL-10 secretion. MRT199665 treatment can block MEF2C S222 phosphorylation in acute myeloid leukemia (AML) cells. MRT199665 (1 nM-100 μM; 48 hours) decreases leukemia growth. MRT199665 (10 nM-1000 nM; 12 hours) leads to a dose-dependent reduction in total and pS222 MEF2C [1][2].

1456858-57-3

C28H31N5O2

469.58

MRT199665

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years