AP20187 (B/B Homodimerizer)

Catalog No.S8487 Batch:S848701

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Technical Data

Formula

C82H107N5O20
Molecular Weight 1482.75 CAS No. 195514-80-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (67.44 mM)
Ethanol 100 mg/mL (67.44 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%Ethanol 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (3.37mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified Ethanol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (3.37mM)
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (3.37mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
Targets
FKBP Casp8
In vitro

In oligodendrocytes, AP20187 treatment increases the expression of PERK-responsive genes encoding CAATT enhancer binding protein homologous protein (CHOP) and growth arrest and DNA damage 34 (GADD34) in a dose-dependent manner. The activity of PERK signalling in oligodendrocytes can be temporally manipulated by the administration of this compound.
In Vivo

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. This compound is also sufficient to activate Fv2E-PERK in oligodendrocytes in the CNS of PLP/Fv2E-PERK mice.

Protocol (from reference)

Cell Assay:

[2]
  • Cell Lines

    Oligodendrocytes

  • Concentrations

    1 nM

  • Incubation Time

    4 h

  • Method

    After 3 d of differentiation, the cells are treated with 1 nM AP20187 or vehicle for 4 h and are then fixed with cold 4% paraformaldehyde in PBS. The cells are blocked with PBS containing 10% goat serum and 0.1% Triton X-100 and incubate overnight with the primary antibody diluted in blocking solution. Appropriate fluorochrome-labeled secondary antibodies are used for detection.
Animal Study:

[2]
  • Animal Models

    PLP/Fv2E-PERK mice

  • Dosages

    0.5 mg/kg, 2 mg/kg, 5 mg/kg

  • Administration

    i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/26840489/
  • https://pubmed.ncbi.nlm.nih.gov/23554479/

Sellecks AP20187 (B/B Homodimerizer) Has Been Cited by 1 Publication

CcGSDMEa functions the pore-formation in cytomembrane and the regulation on the secretion of IL-lβ in common carp (Cyprinus carpio haematopterus) [ Front Immunol, 2022, 13:1110322] PubMed: 36685536

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.