Name | AP20187 |
Synonyms | AP20187 AP-20187 AP 20187 AP20187 (AP-20187 (1S,1'S)-(((2,2'-((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(acetyl))bis(oxy))bis(3, (1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate) (S,2S,2'S)-(1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate) (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[[2-[[[2-[3-[(1R)-3-(3,4-dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]methyl]-3-(dimethylamino)propyl]amino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate |
CAS | 195514-80-8 |
Molecular Formula | C82H107N5O20 |
Molar Mass | 1482.75 |
Solubility | DMSO: ≥ 57 mg/mL |
Storage Condition | -20℃ |
In vitro study | When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent. |
In vivo study | Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) 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. |
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 |
5 mM | 0.013 ml | 0.067 ml | 0.135 ml |
biological activity | AP20187 (B/B Homodimerizer) is a cell-permeable molecule that dimerges FK506 binding protein (FKBP), initiates biological signal transduction cascade and gene expression, or destroys protein-protein interactions. |
target | FKBP homodimerizer |
in vitro study | when LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent. |
in vivo study | Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mices at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mices. AP20187 (B/B Homodimerizer) 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 mices. |