Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 8-10 weeks | $ 1,520.00 | |
50 mg | 8-10 weeks | $ 1,980.00 | |
100 mg | 8-10 weeks | $ 2,500.00 |
Description | 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. |
Targets&IC50 | MELK:29 nM, AMPK α2:10 nM, TBK1:5400 nM, SIK1:110 nM, BRSK2:10000 nM, MARK4:2 nM, IKKε:7700 nM, SIK2:12 nM, SIK3:43 nM, MARK3:3 nM, NUAK1:3 nM, NUAK2:120 nM, MARK1:2 nM, MARK2:2 nM, AMPK α1:10 nM |
In vitro | 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]. |
Molecular Weight | 469.58 |
Formula | C28H31N5O2 |
CAS No. | 1456858-57-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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MRT199665 1456858-57-3 Others MRT-199665 MRT 199665 inhibitor inhibit