Description
QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM, respectively.
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Molecular Formula
C22H20N4O
Chemical Name
4,6-Quinazolinediamine, N4-[2-(4-phenoxyphenyl)ethyl]-
Solubility
DMSO 5 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
EVP4593 inhibits TNF-a production from murine splenocytes stimulated with LPS with IC50 of 7 nM. EVP4593 (300 nM) entails a significant decrease of amplitude of store-operated currents (approximately by 60%), induced by application of 1 μM thapsigargin in Htt138Q cells, thus prevents abnormal store-operated calcium entry. EVP4593 is able to inhibit the activity of channels containing TRPC1 as one of the subunits, but has no effect on homooligomer channels composed exclusively of TRPC1.QNZ (40 nM) completely abolishes the enhancement of neurite number and length evoked by laminin treatment of the schwann cells. QNZ reduces the neurite length by 61.36% of the schwann cells. QNZ significantly inhibits laminin-induced neurite outgrowth. QNZ also greatly diminishes the neurite elongation after 72 hours culture implying that both initial sprouting and longer term growth and extension seen in response to schwann cells seeded on laminin is mediated by NF-κB.QNZ (10 nM) abolishes LPS-induced up-regulation of CSE expression in rat neutrophil.QNZ (100 nM) blocks the induction effects of GRO/KC on K currents in IB4-negative neurons.
In vivo
EVP4593 (1 mg/kg, i.p.) dose-dependently inhibits carrageenin-induced paw edema in rats.
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