| Bioactivity | LOM612 is a potent FOXO relocator, with an EC50 value of 1.5 μM in U2fox RELOC cells[1]. |
| Target | EC50: 1.5 μM (FOXO, in U2fox RELOC cells) |
| Invitro | LOM612 potently activates nuclear translocation of FOXO with an EC50 value of 1.5 μM, and this effect is independent of CRM-1. LOM612 effectively induces translocation of endogenous FOXO3a and FOXO1, and increases the expression of the FOXO target genes p27 and FasL. LOM612 shows no effect on the nuclear export of endogenous NFKB2 transcription factor in U2OS cells. LOM612 is cytotoxic to HepG2 cells, with an IC50 value of 0.64 μM, and does not sensitize non-cancer THLE2 cells (IC50, 2.76 μM)[1]. |
| Name | LOM612 |
| CAS | 2173232-79-4 |
| Formula | C13H10N2O2S |
| Molar Mass | 258.30 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Cautain B, et al. Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling. PLoS One. 2016 Dec 9;11(12):e0167491. |