AP20187

Synonyms: B/B Homodimerizer

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

AP20187 Chemical Structure

AP20187 Chemical Structure

CAS: 195514-80-8

Selleck's AP20187 has been cited by 1 publication

Purity & Quality Control

Batch: S848701 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

AP20187 Related Products

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 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]

Cell Research 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.

In Vivo
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]

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

Chemical Information & Solubility

Molecular Weight 1482.75 Formula

C82H107N5O20

CAS No. 195514-80-8 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (67.44 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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