MRT 199665

Modify Date: 2025-08-25 00:03:06

MRT 199665 Structure
MRT 199665 structure
Common Name MRT 199665
CAS Number 1456858-57-3 Molecular Weight 373.43
Density N/A Boiling Point N/A
Molecular Formula C18H19N3O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MRT 199665


MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.

 Names

Name MRT 199665

 MRT 199665 Biological Activity

Description MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.
References References 1. Clark K, et al. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91. 2. Darling NJ, et al. Biochem J. 2017 Feb 15;474(4):521-537. 3. Huang HT, et al. Elife. 2017 Sep 19;6. pii: e26693. View Related Products by Target Salt Inducible Kinase (SIK)

 Chemical & Physical Properties

Molecular Formula C18H19N3O4S
Molecular Weight 373.43
InChIKey OFIFLUFVENTCNZ-QHCPKHFHSA-N
SMILES CC1(C)C(=O)N(C2CCc3c(O)cccc32)c2nc(Nc3cccc(CN4CCCC4)c3)ncc21
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