NF-kB Activation Inhibitor VIII, EVP4593 (SOC Inhibitor, Neuronal Store-Operated Calcium Entry Inhibitor, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, TRPC1 Inhibitor)

Size

£358.00

SKU:: 217588
Molecular Weight:: 356.4
Purity:: ~98% (HPLC)
Storage Conditions:: -20°C
Supplier:: United States Biological
Format:: Supplied as a yellow powder.
Extra Details:: 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.