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AP20187 

Cat. No.: HY-13992 Purity: 99.80%
Data Sheet SDS Handling Instructions

AP20187 is a cell-permeable molecule used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.

For research use only. We do not sell to patients.
AP20187 Chemical Structure

AP20187 Chemical Structure

CAS No. : 195514-80-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2544 In-stock
1 mg USD 360 In-stock
5 mg USD 960 In-stock
10 mg USD 1560 In-stock
25 mg USD 2280 In-stock
50 mg USD 3120 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AP20187 is a cell-permeable molecule used to dimerize FK506-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 of PLP/Fv2E-PERK mice 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 of PLP/Fv2E-PERK mice[2].

References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

AP20187 is dissolved in PBS[2].

For the in vitro study, 16 h after ADV infection, cells are treated with R1881 (10 nM), AP20187 (10 nM), both, or neither for 8 h. Cells are then rinsed with PBS and fixed with 4% paraformaldehyde for 1 h at room temperature. After rinsing with PBS, cells are incubated in ice-cold permeabilization solution (0.1% Triton X-100, 0.1% sodium citrate) for 2 min at 0°C. Cells are rinsed with PBS and stained with TUNEL reaction mixture for 60 min at 37°C. After another PBS wash, cells are incubated with Converter-AP for 30 min at 37°C. Cells are rinsed and incubated with substrate 5-bromo-4-chloro-3-indolyl phosphate/nitroblue tetrazolium for 30 min. After a final PBS rinse (repeated twice), cells are microphotographed[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

AP20187 is dissolved in 100% ethanol at a concentration of 62.5 mg/mL and stored (20°C). Then treatment solutions is freshly prepared from a dilution of 1.25 mg/mL consisting of 4% ethanol, 10% PEG-400, and 2% Tween-20 in water[2].

Mice[2]
To activate the transgene Fv2E-PERK in oligodendrocytes, PLP/Fv2E-PERK transgenic mice are given intraperitoneal injections of AP20187 daily at a dose of 0.5 mg/kg, 2 mg/kg, or 5 mg/kg. Lyophilized AP20187 is dissolved in 100% ethanol at a concentration of 62.5 mg/mL stock solution and stored at −20°C. Injection solutions consist of 4% ethanol, 10% PEG-400, and 2% Tween-20 in water. The transgenic mice receiving only the vehicle (4% ethanol, 10% PEG-400, 2% Tween-20 in water) served as controls. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1482.75

Formula

C₈₂H₁₀₇N₅O₂₀

CAS No.

195514-80-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 57 mg/mL

AP20187 is dissolved in 4% ethanol, 10% PEG-400, 1.75% Tween-20 in H2O[3].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

Purity: 99.80%

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AP20187
Cat. No.:
HY-13992
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