| Bioactivity | 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, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively[1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells[2]. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370[3]. | ||||||||||||
| Invitro | MRT199665 (1 μM; pre-treated for 1 h) increases LPS (100 ng/mL; stimulated for up to 24 h)-stimulated IL-10 mRNA and Nurr77 mRNA production, and IL-10 secretion[1]. MRT199665 (1 nM-100 μM; 48 hours) reduces leukemia growth[2].MRT199665 treatment can block MEF2C S222 phosphorylation in acute myeloid leukemias (AML) cells.MRT199665 (10 nM-1000 nM; 12 hours) leads to a dose-dependent reduction in total and pS222 MEF2C. MRT199665 also causes a decrease of total MEF2C protein[2]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| Name | MRT199665 | ||||||||||||
| CAS | 1456858-57-3 | ||||||||||||
| Formula | C28H31N5O2 | ||||||||||||
| Molar Mass | 469.58 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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MRT199665
CAS: 1456858-57-3 F: C28H31N5O2 W: 469.58
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
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