MRT199665
CAS No. : 1456858-57-3
| Size | Price | Stock |
|---|---|---|
| 5mg | $580 | In-stock |
| 10mg | $950 | In-stock |
| 25mg | $1950 | In-stock |
| 50mg | $3350 | In-stock |
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| Cat. No. : | HY-120877 |
| M.Wt: | 469.58 |
| Formula: | C28H31N5O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
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].
In Vitro: 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].
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