产品说明
一般描述
A cell-permeable, potent, and selective blocker of necroptosis (EC50 = 494 nM in FADD-deficient Jurkat cells treated with TNF-α), a nonapoptotic necrotic cell death pathway mediated by death-domain receptors (DRs) that offers neuroprotection in a murine model of ischemic brain injury. Exhibits no effect on DR-induced apoptosis. Also acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect of RIP2 kinase activity. Nec-1 target appears to be a critical common necroptotic step upstream of execution events and downstream of DRs. Inactive control, Nec-1i, is also available (Cat. No. 480066). Also available as a 25 mM solution in DMSO (Cat. No. 505224).
A cell-permeable, potent, and selective blocker of necroptosis (EC50 = 494 nM in FADD-deficient Jurkat cells treated with TNF-α), a nonapoptotic necrotic cell death pathway mediated by death-domain receptors (DRs) that offers neuroprotection in a murine model of ischemic brain injury. Exhibits no effect on DR-induced apoptosis. Also acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect of RIP2 kinase activity. Nec-1 target appears to be a critical common necroptotic step upstream of execution events and downstream of DRs. Inactive control, Nec-1i, is also available (Cat. No. 480066).
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
Blocker of necroptosis
Reversible: no
Product competes with ATP.
EC50 = 494 nM in blocking necrosis in FADD-deficient Jurkat cells treated with TNF-α
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Degterev, A., et al. 2013. Nat. Chem. Biol.9, 192.
Degterev, A., et al. 2012. Cell Death Differ.20, 366.
Christofferson, D.E., et al. 2012. Cell Death Dis.3, e320.
Takahashi, N., et al. 2012. Cell Death Dis.3, e437.
Degterev, A., et al. 2008. Nat. Chem. Biol.4, 313.
Degterev, A., et al. 2005. Nat. Chem. Biol.1, 112.
Muller, A.J., et al. 2005. Nat. Med.11, 312.
Teng, X., et al. 2005. Bioorg. Med. Chem. Lett.15, 5039.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C13H13N3OS |
| 分子量 | 259.33 |
| MDL编号 | MFCD00056916 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | crystalline solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | yellow |
| 溶解性 | DMSO: 10 mg/mL methanol: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| InChI | 1S/C13H13N3OS/c1-16-12(17)11(15-13(16)18)6-8-7-14-10-5-3-2-4-9(8)10/h2-5,7,11,14H,6H2,1H3,(H,15,18) |
| InChI key | TXUWMXQFNYDOEZ-UHFFFAOYSA-N |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
