General description

A cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-κB activation in Jurkat cells (IC₅₀ = 11 nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1 mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300 nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30 nM to 3 µM, which is consistent with TRPC1 knockdown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100 µM to 400 µM.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wu, J., et al. 2011. Chem Biol.18, 777.Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 383.Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 3869.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)