AP20187

AP20187 is a chemical inducer of dimerization (CID) for FK506 binding protein (FKBP) fusion proteins. 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. 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. 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 p16Ink4a-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. AP20187 delays tumorigenesis and reduces glomerulosclerosis and kidney dysfunction in the same mouse model.Formal Name: 2-piperidinecarboxylic acid, (2S,2'S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2,2'-[[2-[(dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester. CAS Number: 195514-80-8. Synonyms: B/B Homodimerizer. Molecular Formula: C82H107N5O20. Formula Weight: 1482.8. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, Ethanol: 2 mg/ml, PBS (pH 7.2): insol. SMILES: O=C(N1[C@@H](CCCC1)C(O[C@@H](C2=CC(OCC(NCC(CN(C)C)CNC(COC3=CC([C@@H](CCC4=CC(OC)=C(C=C4)OC)OC([C@H]5N(CCCC5)C([C@H](C6=CC(OC)=C(C(OC)=C6)OC)CC)=O)=O)=CC=C3)=O)=O)=CC=C2)CCC7=CC(OC)=C(C=C7)OC)=O)[C@H](C8=CC(OC)=C(C(OC)=C8)OC)CC. InChi Code: InChI=1S/C82H107N5O20/c1-15-61(57-43-71(98-9)77(102-13)72(44-57)99-10)79(90)86-37-19-17-27-63(86)81(92)106-65(33-29-52-31-35-67(94-5)69(39-52)96-7)55-23-21-25-59(41-55)104-50-75(88)83-47-54(49-85(3)4)48-84-76(89)51-105-60-26-22-24-56(42-60)66(34-30-53-32-36-68(95-6)70(40-53)97-8)107-82(93)64-28-18-20-38-87(64)80(91)62(16-2)58-45-73(100-11)78(103-14)74(46-58)101-12/h21-26,31-32,35-36,39-46,54,61-66H,15-20,27-30,33-34,37-38,47-51H2,1-14H3,(H,83,88)(H,84,89)/t61-,62-,63-,64-,65+,66+/m0/s1. InChi Key: NSBGUMKAXUXKGI-BPNHAYRBSA-N.