Ferritin PROTAC DeFer-2

Ferritin PROTAC DeFer-2 is a proteolysis-targeting chimera (PROTAC) containing oleic acid (Cay-90260, Cay-24659), which binds to ferritin dimers, conjugated to von Hippel-Lindau ligand (VHL ligand 1, Cay-21591), which binds to VHL E3 ligase, via an alkyl linker. It induces ferritin degradation in B16/F10 murine melanoma cells when used at a concentration of 0.5 µM, an effect not induced by a negative control with an inverted VHL ligand 1 stereocenter, indicating that the E3 ligase activity of VHL ligand 1 is required for this effect. Ferritin PROTAC DeFer-2 (5 µM) increases intracellular levels of free iron and induces pyroptosis in B16/F10 cells. Ferritin PROTAC De-Fer-2 (10 mg/kg) encapsulated in albumin nanoparticles reduces tumor growth and increases survival in a B16/F10 murine melanoma model.Formal Name: (2S,4R)-1-((S)-3,3-dimethyl-2-(4-oleamidobutanamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide. Synonyms: Ferritin Proteolysis-targeting Chimera DeFer2. Molecular Formula: C44H69N5O5S. Formula Weight: 780.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 10 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): Slightly. SMILES: CC1=C(C2=CC=C(CNC([C@@H](N3C([C@@H](NC(CCCNC(CCCCCCC/C=C\CCCCCCCC)=O)=O)C(C)(C)C)=O)C[C@H](C3)O)=O)C=C2)SC=N1. InChi Code: InChI=1S/C44H69N5O5S/c1-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-22-38(51)45-28-21-23-39(52)48-41(44(3,4)5)43(54)49-31-36(50)29-37(49)42(53)46-30-34-24-26-35(27-25-34)40-33(2)47-32-55-40/h13-14,24-27,32,36-37,41,50H,6-12,15-23,28-31H2,1-5H3,(H,45,51)(H,46,53)(H,48,52)/b14-13-/t36-,37+,41-/m1/s1. InChi Key: FOJJJSRIPHLZFB-HJBYGEKRSA-N.