616404
Tpl2 Kinase Inhibitor II - CAS 1186649-59-1 - Calbiochem
Synonym(s):
4-(Cycloheptylamino)-6-(pyridin-3-yl-methylamino)-3-cyano-[1,7]-naphthyridine, hydrate, Tumor Progression Locus 2 Kinase Inhibitor II
assay
≥97% (HPLC)
form
solid
color
pale yellow
solubility
ethanol: 1 mg/mL
DMSO: 50 mg/mL
General description
A cell-permeable naphthyridine-cyclohexyl Tpl2 Kinase Inhibitor (Cat. No. 616373) analog that acts as a potent ATP-competitive Tpl2 inhibitor (IC50 = 160 nM) with little activity (IC50 >20 μM) against EGFR, Src, MEK, p38, PKA, PKC, or S6. Reported to block LPS-induced TNF-α production both in vitro (IC50 = 0.5 and 4.5 μM using human monocytes and whole blood, respectively) and in rats in vivo (10 mg/kg, i.p.).
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Storage Class
10-13 - German Storage Class 10 to 13
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Neelu Kaila et al.
Bioorganic & medicinal chemistry, 15(19), 6425-6442 (2007-08-01)
We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identification of 4-alkylamino-[1,7]naphthyridine-3-carbonitriles. These compounds show
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