MDL | - |
---|---|
Molecular Weight | 1482.75 |
Molecular Formula | C82H107N5O20 |
SMILES | COC1=C(OC)C=C(CC[C@H](C2=CC=CC(OCC(NCC(CN(C)C)CNC(COC3=CC=CC([C@H](OC([C@H]4N(C([C@@H](CC)C5=CC(OC)=C(OC)C(OC)=C5)=O)CCCC4)=O)CCC6=CC(OC)=C(OC)C=C6)=C3)=O)=O)=C2)OC([C@@H]7CCCCN7C([C@H](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)C=C1 |
AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein ( FKBP ) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
FKBP homodimerizer [1]
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
Ethanol : 150 mg/mL ( 101.16 mM ; Need ultrasonic)
DMSO : ≥ 57 mg/mL ( 38.44 mM )
* "≥" means soluble, but saturation unknown.
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 0.6744 mL | 3.3721 mL | 6.7442 mL |
5 mM | 0.1349 mL | 0.6744 mL | 1.3488 mL |
10 mM | 0.0674 mL | 0.3372 mL | 0.6744 mL |
Add each solvent one by one: 10% EtOH >> 90% (20% SBE-β-CD in saline)
Solubility: 6 mg/mL (4.05 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution
Add each solvent one by one: 4% ethanol >> 10% PEG-400 >> 2% Tween-80 >> 84%water.
Solubility: 2.4 mg/mL (1.62 mM); Clear solution; Need ultrasonic