Antibodies
QNZ (EVP4593)
- 貨號 Cat. No.
- S4902
- 規格 Size
- 5mgã€25mg
- 品牌 Brand
- Selleckchem
Description
QNZ (EVP4593)
Catalog No.S4902
QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| 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. | |||||
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| Targets | NF-κB | |||||
| IC50 | 11 nM [1] | |||||
| In vitro | EVP4593 inhibits TNF-a production from murine splenocytes stimulated with LPS with IC50 of 7 nM. [1]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. [2] 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. [3] QNZ (10 nM) abolishes LPS-induced up-regulation of CSE expression in rat neutrophil. [4] QNZ (100 nM) blocks the induction effects of GRO/KC on K currents in IB4-negative neurons. [5] | |||||
| In vivo | EVP4593 (1 mg/kg, i.p.) dose-dependently inhibits carrageenin-induced paw edema in rats. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| NF-κB assay | Human Jurkat T cells are cultured at 37℃ in a 5% CO2 atmosphere in RPMI1640 containing 10% FCS, 100 U/mL of penicillin, and 100 μg/mL of streptomycin. The cells are plated in 6-well plates (2×106/well) and transiently transfected using the SuperFect Transfection Reagent with 1 μg of pNFκB-Luc. After transfection, the cells are cultured at 37℃ overnight. They are then collected, resuspended in fresh medium, and plated in 96-well plates (2×105/well). EVP4593 is dissolved in DMSO and added at the appropriate concentrations to the 96-well plates containing the cells, and the plates are then incubated at 37℃ for 1 hour. For induction of transcription, 10 ng/mL of PMA and 100 μg/mL of PHA are added to each well, and the cells are incubated for an additional 6 hours at 37℃. The culture media are removed, and cell lysis buffer containing luciferase substrate is added to each well. The each portion is transferred to a black 96-well plate, and then luminescence is immediately measured with a Packard Topcount. The 50% inhibitory concentration (IC50) values are calculated by a nonlinear regression method. |
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Animal Study: [1]
| Animal Models | male SD rats with carrageenin induced paw edema |
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| Dosages | 1 mg/kg |
| Administration | intraperitoneal injection |
| Solubility | 0.5% hyroxyethylcellulose., 30 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 356.42 |
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| Formula | C22H20N4O |
| CAS No. | 545380-34-5 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 5 mg/mL (14 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 0.5% hyroxyethylcellulose., | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4,6-Quinazolinediamine, N4-[2-(4-phenoxyphenyl)ethyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.35642 | 3.5642 | 7.1284 | 10.6926 |
