| 产品描述: | AP20187 (B/B Homodimerizer, HY-13992) 是一种二聚化的化学诱导剂,可激活 FKBP-Casp8 |
| 靶点: |
FKBP; Casp8;Others |
| 体外研究: |
In oligodendrocytes, AP20187 treatment increases the expression of PERK-responsive genes encoding CAATT enhancer binding protein homologous protein (CHOP) and growth arrest and DNA damage 34 (GADD34) in a dose-dependent manner. The activity of PERK signaling in oligodendrocytes can be temporally manipulated by the administration of AP20187 |
| 体内研究: |
AP20187 treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2E-PERK mice. AP20187 is also sufficient to activate Fv2E-PERK in oligodendrocytes in the CNS of PLP/Fv2E-PERK mice. |
| 细胞实验: |
Cell lines: Oligodendrocytes Concentrations: 1 nM Incubation Time: 4 h Method: After 3 d of differentiation, the cells are treated with 1 nM AP20187 or vehicle for 4 h and are then fixed with cold 4% paraformaldehyde in PBS. The cells are blocked with PBS containing 10% goat serum and 0.1% Triton X-100 and incubate overnight with the primary antibody diluted in blocking solution. Appropriate fluorochrome-labeled secondary antibodies are used for detection. |
| 动物实验: |
Animal Models: PLP/Fv2E-PERK mice Dosages: 0.5 mg/kg, 2 mg/kg, 5 mg/kg Administration: i.p. |
| 参考文献: |
1. Darren J Baker, et al. Naturally occurring p16(Ink4a)-positive cells shorten healthy lifespan. Nature . 2016 Feb 11;530(7589):184-9. 2. Wensheng Lin, et al. Oligodendrocyte-specific activation of PERK signaling protects mice against experimental autoimmune encephalomyelitis. J Neurosci . 2013 Apr 3;33(14):5980-91. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
0.674 ml |
3.372 ml |
6.744 ml |
| 5 mM |
0.135 ml |
0.674 ml |
1.349 ml |
| 10 mM |
0.067 ml |
0.337 ml |
0.674 ml |
| 50 mM |
0.013 ml |
0.067 ml |
0.135 ml |
|
| 注意: |
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