(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKalpha1/AMPKalpha2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370[1][2][3].
Molekulargewicht:
469.58
Reinheit:
98.70
Formel:
C28H31N5O2
Target-Kategorie:
AMPK,Apoptosis,MARK,Salt-inducible Kinase (SIK)
Anwendungsbeschreibung:
MCE Product type: Reference compound
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