MRT199665 |
| Catalog No.GC60256 |
MRT199665는 MARK1/MARK2/MARK3/MARK14, AMPKα1에 대해 IC50이 2/2/3/2 nM, 10/10 nM 및 110/12/43 nM인 강력하고 ATP 경쟁적인 선택적 MARK/SIK/AMPK 억제제입니다. /AMPKα2 및 SIK1/SIK2/SIK3. MRT199665는 MEF2C 활성화 인간 급성 골수성 백혈병(AML) 세포에서 세포자멸사를 유발합니다. MRT199665는 S370에서 SIK 기질 CRTC3의 인산화를 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1456858-57-3
Sample solution is provided at 25 µL, 10mM.
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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].
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: OCI-AML2 and MOLM-13 cells
[1]. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91. [2]. Brown FC, et al. MEF2C Phosphorylation Is Required for Chemotherapy Resistance in Acute Myeloid Leukemia. Cancer Discov. 2018 Apr;8(4):478-497. [3]. Hutchinson LD, et al. Salt-inducible kinases (SIKs) regulate TGFβ-mediated transcriptional and apoptotic responses.Cell Death Dis. 2020 Jan 22;11(1):49.
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