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Tpl2/MAP3K8 inhibitor 32

Chemical Structure : Tpl2/MAP3K8 inhibitor 32

CAS No.: 1984784-10-2

Tpl2/MAP3K8 inhibitor 32 (COT kinase inhibitor 32)

Catalog No.: PC-22733Not For Human Use, Lab Use Only.

Tpl2/MAP3K8 inhibitor 32 is a potent, selective inhibitor of cancer osaka thyroid (COT) kinase (Tpl2, MAP3K8) with IC50 of 6 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Tpl2/MAP3K8 inhibitor 32 is a potent, selective inhibitor of cancer osaka thyroid (COT) kinase (Tpl2, MAP3K8) with IC50 of 6 nM.
Tpl2/MAP3K8 inhibitor 32 inhibits pERK and TNFα production in PBMCs with IC50 of 60 nM for both.
Tpl2/MAP3K8 inhibitor 32 demonstrates potent inhibition of the formation of the pro-inflammatory cytokine interleukin-1β (IC50: 0.2 μM) in uric-acid, stimulated macrophages.
Tpl2/MAP3K8 inhibitor 32 (5-15 mg/kg) shows a clear amelioration of inflammatory events in the dog uric acid-induced synovitis model.

Physicochemical Properties

M.Wt 516.61
Formula C30H28N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(1-morpholinopropan-2-yl)-6-(8-(pyridin-4-yl)-1H-imidazo[4,5-c][1,7]naphthyridin-1-yl)quinolin-2-amine

References

1. Ralf Glatthar, et al. J Med Chem. 2016 Aug 25;59(16):7544-60.

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