General description
A cell-permeable naphthyridine compound that acts as a potent, reversible, and ATP-competitive inhibitor of Tpl2 kinase (IC50 = 50 nM). Displays significant selectivity over other related kinases (IC50 = 5, >40, 110, 180, >400 and >400 µM for EGFR, MEK, MK2, p38, Src, and PKC, respectively). Shown to inhibit LPS-induced TNF-α production both from primary human monocytes and in whole blood (IC50 = 700 nM and 8.5 µM, respectively).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Tpl2 Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 50 nM against Tpl2 kinase
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Gavrin, L.K., et al. 2005. Bioorg. Med. Chem. Lett.15, 5288.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 616373-1MG