QNZ, NFkB inhibitor / Store-operated calcium entry

Product Details

Formal Name: 4-N-[2-(4-Phenoxyphenyl)ethyl]quinazoline-4,6-diamine

Alternate Names: EVP4593

Molecular Formula: C₂₂H₂₀N₄O

Formula Weight: 356.42

CAS Number: 545380-34-5

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 20 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

NFkB inhibitor / Store-operated calcium entry

Functions

Originally described as a potent inhibitor of NF-κB activation (IC50 = 11 n) and TNF-α production (IC50 = 7 nM). Indirectly inhibits the NF-κB pathway via inhibition of store-operated calcium entry (SOC) and displayed neuroprotective effects in transgenic fly and mouse models of Huntington’s disease. Its target has been postulated to be heteromeric calcium channels containing TRPC1 as one of the subunits. QNZ reduced synaptic neuronal SOC and rescued dendritic spine loss in YAC128 striatal medium spiny neurons. QNZ has also been identified as a potent and selective inhibitor of mitochondrial complex I (IC50 = 25 nM complex 1 from Y.lipolytica; IC50 = 14 nm complex 1 from Bos Taurus heart mitochondria). QNZ decreased PSEN1ΔE9-mediated nSOCE upregulation and rescued mushroom spines in PSEN1ΔE9-expressing neurons, which are linked to familial Alzheimer’s disease.

Application Procedures

First dissolved in DMSO (up to 20 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)