"目录号: HY-13992
PI3K/Akt/mTOR-
AP20187 是一种细胞渗透性分子，使FK506结合蛋白 (FKBP)二聚化，启动生物信号传导级联反应和基因表达，或破坏蛋白-蛋白之间相互作用。
mTOR
相关产品
Rapamycin-Everolimus-AP1903-INK-128-BEZ235-Torin 1-AZD-8055-MHY1485-PP 242-LY3023414-AZD2014-PF-04691502-Temsirolimus-Torin 2-GSK2126458-
生物活性
Description
AP20187 is a cell-permeable molecule used to dimerizeFK506-binding protein(FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
IC50& Target
FKBP homodimerizer[1]
In Vitro
When LNCaP cells are treated with AP20187 (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent[2].
In Vivo
Real-time PCR analysis shows that AP20187 (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS ofPLP/Fv2E-PERKmice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord ofPLP/Fv2E-PERKmice[2].
References
[1].Ahmed S, et al. Photocleavable dimerizer for the rapid reversal of molecular trap antagonists. J Biol Chem. 2014 Feb 21;289(8):4546-52.
[2].Lin W, et al. Oligodendrocyte-specific activation of PERK signaling protects mice against experimental autoimmune encephalomyelitis. J Neurosci. 2013 Apr 3;33(14):5980-91.
[3].Haas ME, et al. The Role of Proprotein Convertase Subtilisin/Kexin Type 9 in Nephrotic Syndrome-Associated Hypercholesterolemia. Circulation. 2016 Jul 5;134(1):61-72.