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MRT 199665

CAT: 0013-GTR19237288-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19237288-01Size:5 mg
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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. (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.MRT199665 (1 nM-100 μM; 48 hours) reduces leukemia growth.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.
CAS Number
1456858-57-3
Product Name Alternative
MRT199665
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 125 mg/mL (266.20 mM)
Smiles
O=C1C (C) (C) C2=CN=C (S (=O) (C) =O) N=C2N1[C@H]3CCC4=C3C=CC=C4O
Molecular Formula
C18H19N3O4S
Molecular Weight
373.43
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
7-[ (1S) -4-Hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2- (methylsulfonyl) -5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

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