[CAS NO. 852391-19-6] Necrostatin2
PRODUCTS SPECIFICATIONS [852391-19-6]
DESCRIPTION [852391-19-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 277.71 |
| Molecular Formula | C13H12ClN3O2 |
| SMILES | ClC1=C2C(C(C[C@@H]3C(N(C)C(N3)=O)=O)=CN2)=CC=C1 |
3 Publications Citing Use of MCE
Summary
Necrostatin 2 is a potent necroptosis inhibitor. EC 50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
In Vitro
Evaluation of necroptosis inhibitory activity is performed using a FADD-deficient variant of human Jurkat T cells treated with TNF-α. Utilizing these conditions the cells efficiently undergo necroptosis, which is completely and selectively inhibited by Necrostatin 2 (EC 50 =50 nM). Necrostatin 2 shows activity in a broad range of necroptosis cellular systems [1] . Necrostatin 2 at 30 μM completely protects L929 cells from TNF-α-induced necroptosis. In addition to TNF-α, the pan-caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone (zVAD.fmk) has also been found to induce necrosis in L929 cells, which is efficiently inhibited by Necrostatin 2 [2] . EC 50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 360.09 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.6009 mL | 18.0044 mL | 36.0088 mL |
| 5 mM | 0.7202 mL | 3.6009 mL | 7.2018 mL |
| 10 mM | 0.3601 mL | 1.8004 mL | 3.6009 mL |
References
- [1] Teng X, et al. Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40.
- [2] Jagtap PG, et al. Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886-95.
- [3] Teng X, et al. Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039-44.
- [4] Takahashi N, et al. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models. Cell Death Dis. 2012 Nov 29;3:e437.
