A cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-kB activation in Jurkat cells (IC50=11nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1mg/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 300nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30nM to 3uM, which is consistent with TRPC1 knocown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100uM to 400uM.
Formula:C22H20N4O
Molecular Weight:356.4
Solubility:DMSO (100mg/ml clear, yellow solution)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
