| Description | AP20187 (B/B Homodimerizer) is a cell-permeable compound employed to dimerize FK506-binding protein (FKBP) fusion proteins, thereby initiating biological signaling cascades, gene expression, or disrupting protein-protein interactions. |
| In vitro | 当LNCaP细胞用AP20187（B/B Homodimerizer）（100 nM）处理时，ro-iCaspase-9的水平显著降低。然而，较小的活化caspase-9变得明显[2]。 |
| In vivo | AP20187处理显著缓解了这些小鼠EAE引起的髓磷脂损伤。AP20187（B/B Homodimerizer）处理在PLP/Fv2E-PERK小鼠腰椎脊髓的脱髓鞘损伤中，显著减少了退化轴突的数量，并增加了轴突的密度[2]。实时PCR分析表明，AP20187（B/B Homodimerizer）（0.5 mg/kg、2 mg/kg或5 mg/kg）处理在PLP/Fv2E-PERK小鼠的中枢神经系统中，显著增加了CHOP mRNA的水平，在PID12时。 |
| Synonyms | B/B Homodimerizer |
| molecular weight | 1482.75 |
| Molecular formula | C82H107N5O20 |
| CAS | 195514-80-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/mL (37.09 mM) Ethanol: 130 mg/mL (87.67 mM), Sonication is recommended. |
| 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. |