The NF-κB Activation Inhibitor VIII, EVP4593 controls the biological activity of NF-κB. This small molecule/inhibitor is primarily used for Neuroscience applications.
Synonyme(s) :
CRAC Channel Inhibitor IV, EVP4593, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
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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.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
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.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
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International journal of molecular sciences, 23(24) (2022-12-24)
Quinazoline derivatives have various pharmacological activities and are widely used in clinical practice. Here, we reviewed the proposed mechanisms of the physiological activity of the quinazoline derivative EVP4593 and perspectives for its clinical implication. We summarized the accumulated data about
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