Antibodies
NSC 319726
- 貨號 Cat. No.
- S7149
- 規格 Size
- 5mgã€25mg
- 品牌 Brand
- Selleckchem
Description
NSC 319726
Catalog No.S7149
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, withIC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells. | |||||
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| Targets | p53(R175) | |||||
| IC50 | 8 nM [1] | |||||
| In vitro | NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells, shows 10- to 100-fold selectivity over the other hotspot p53 mutants. NSC319276 induces p53(R175)-mutant-dependent apoptosis. NSC319726 treatment induces a WT-like conformational change in the p53(R175) mutant protein that restores sequence-specific p53 transcription. The activity of NSC319726 depends on the zinc ion chelating properties of the compound as well as redox changes. [1] | |||||
| In vivo | NSC319726 (5mg/kg, 7days) exhibits greater toxicity for p53(R172H/R172H) mice, with only 30% survival, as compared to 100% survival for p53+/+ and p53-/- mice. NSC319726 inhibits the growth of TOV112D-p53(R175H) xenografts, but not H460 (p53+/+) and MDAMB468-p53(R273W) xenografts. [1] | |||||
| Features | An allele-specific p53 mutant reactivator. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| MTS | 5,000 cells of TOV112D cells (5,000 cells/well, in 100 ml culture) are cultured in 96-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compounds. The growth is measured by MTS reagent and Victor Plate reader instrument after incubation for 3 days. |
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Cell Assay: [1]
| Cell lines | MEF with p53 mutations |
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| Concentrations | ~10 μM |
| Incubation Time | 3 days |
| Method | Viability assays are done. The cells (5×104 cells/well, in 1 ml culture) are cultured in a 12-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compound. The growth is measured by Guava ViaCount reagent and Guava PCA instrument after incubation for 3 days. |
Animal Study: [1]
| Animal Models | p53+/+, p53-/- and p53R172H knockin mice |
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| Dosages | 5-10 mg/kg/day, up to 7 days |
| Administration | i.p. |
References
Chemical Information
| Molecular Weight (MW) | 234.32 |
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| Formula | C11H14N4S |
| CAS No. | 71555-25-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 19 mg/mL (81 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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 | 1-Azetidinecarbothioic acid, 2-[1-(2-pyridinyl)ethylidene]hydrazide |
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