AP20187

AP20187 is a chemical inducer of dimerization (CID) for FK506 binding protein (FKBP) fusion proteins.¹ It increases expression of the genes encoding DNA damage-inducible transcript 3 (Ddit3) and growth arrest and DNA damage-inducible protein 34 (Gadd34) in primary mouse neonatal glial cells when used at a concentration of 0.1 nM.² It increases apoptosis induced by adenoviral vectors expressing conditional caspase-1 (Ad-G/iCasp1) in LNCaP and PC3 human prostate, as well as TRAMP-C2 and TRAMP-C2G murine prostate, cancer cells in a concentration-dependent manner.¹ AP20187 (2 mg/kg), when used in combination with Ad-G/iCasp1, induces apoptosis and reduces tumor volume in a TRAMP-C2 murine prostate cancer model. It induces apoptosis in p16^Ink4a-positive senescent cells and increases lifespan in ATTAC transgenic mice expressing FKBP-Casp8 and GFP when administered at a dose of 2 µg/g twice per week.³ AP20187 delays tumorigenesis and reduces glomerulosclerosis and kidney dysfunction in the same mouse model.

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1. Shariat, S.F., Desai, S., Song, W., et al. Adenovirus-mediated transfer of inducible caspases: A novel "death switch" gene therapeutic approach to prostate cancer. Cancer Res. 61(6), 2562-2571 (2001).

2. Lin, W., Lin, Y., Li, J., et al. Oligodendrocyte-specific activation of PERK signaling protects mice against experimental autoimmune encephalomyelitis. J. Neurosci. 33(14), 5980-5991 (2013).

3. Baker, D.J., Childs, B.G., Durik, M., et al. Naturally occurring p16Ink4a-positive cells shorten healthy lifespan. Nature 530(7589), 184-189 (2016).