AP20187

Catalog No.S8487 Synonyms: B/B Homodimerizer

For research use only.

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

AP20187 Chemical Structure

CAS No. 195514-80-8

Purity & Quality Control

Choose Selective FKBP Inhibitors

Biological Activity

Description AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
Targets
FKBP [1] Casp8 [1]
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 signaling in oligodendrocytes can be temporally manipulated by the administration of AP20187.[2]

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. AP20187 is also sufficient to activate Fv2E-PERK in oligodendrocytes in the CNS of PLP/Fv2E-PERK mice.[2]

Protocol (from reference)

Cell Research:

[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 Research:

[2]

  • Animal Models: PLP/Fv2E-PERK mice
  • Dosages: 0.5 mg/kg, 2 mg/kg, 5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 1482.75
Formula

C82H107N5O20

CAS No. 195514-80-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(C1=CC(=C(C(=C1)OC)OC)OC)C(=O)N2CCCCC2C(=O)OC(CCC3=CC(=C(C=C3)OC)OC)C4=CC(=CC=C4)OCC(=O)NCC(CNC(=O)COC5=CC=CC(=C5)C(CCC6=CC(=C(C=C6)OC)OC)OC(=O)C7CCCCN7C(=O)C(CC)C8=CC(=C(C(=C8)OC)OC)OC)CN(C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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