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481417 Sigma-Aldrich

CRAC Channel Inhibitor IV, EVP4593 - Calbiochem

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: CRAC Channel Inhibitor IV, EVP4593 - Calbiochem, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor

  • Empirical Formula (Hill Notation) C22H20N4O

  • Molecular Weight 356.42

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Properties

Quality Level   100
assay   ≥98% (HPLC)
form   powder
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   yellow
solubility   DMSO: 100 mg/mL, clear, yellow
shipped in   ambient

Description

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

5 mg in Glass bottle

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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