1456858-57-3

1456858-57-3 structure

Name: MRT 199665
Chemical Name: MRT 199665
CAS Number: 1456858-57-3
Molecular Formula: C₁₈H₁₉N₃O₄S
Molecular Weight: 373.43
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2020-01-11 18:35:50
Modify Date: 2024-01-08 20:07:49
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.

Name	MRT 199665

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)

Molecular Formula	C₁₈H₁₉N₃O₄S
Molecular Weight	373.43