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
Preparation Note
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
Disclaimer
Toxicity: Irritant (B)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 10 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | Fc1c(cc(cc1)Nc2c3c(ncc2C#N)cnc(c3)NCc4cnccc4)Cl |
| InChI | 1S/C21H14ClFN6/c22-17-6-15(3-4-18(17)23)29-21-14(8-24)11-26-19-12-28-20(7-16(19)21)27-10-13-2-1-5-25-9-13/h1-7,9,11-12H,10H2,(H,26,29)(H,27,28) |
| InChI key | NMEUKWOOQOHUNA-UHFFFAOYSA-N |
