1456858-57-3
Chemical Structure
MRT199665
- CAS No.: 1456858-57-3
- Formula:C28H31N5O2
- Molecular Weight:469.58
IUPAC Name: (S)-7-(4-hydroxy-2,3-dihydro-1H-inden-1-yl)-5,5-dimethyl-2-((3-(pyrrolidin-1-ylmethyl)phenyl)amino)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one
InChIKey: OFIFLUFVENTCNZ-QHCPKHFHSA-N
SMILES: O=C1C(C)(C)C2=CN=C(NC3=CC=CC(CN4CCCC4)=C3)N=C2N1[C@H]5CCC6=C5C=CC=C6O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MRT199665 | 99.85% | 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. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Brown FC, et al. MEF2C Phosphorylation Is Required for Chemotherapy Resistance in Acute Myeloid Leukemia. Cancer Discov. 2018 Apr;8(4):478-497. [Content Brief]
- [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. [Content Brief]
Keywords
