481417
CRAC Channel Inhibitor IV, EVP4593
The NF-κB Activation Inhibitor VIII, EVP4593 controls the biological activity of NF-κB. This small molecule/inhibitor is primarily used for Neuroscience applications.
Synonym(s):
CRAC Channel Inhibitor IV, EVP4593, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C22H20N4O
Molecular Weight:
356.42
MDL number:
UNSPSC Code:
12352200
Recommended Products
Quality Level
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 100 mg/mL, clear, yellow
shipped in
ambient
storage temp.
2-8°C
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.
Packaging
Packaged under inert gas
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 383.
Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 3869.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Dmitriy A Grekhnev et al.
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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