| Description | OGT 2115 is an inhibitor of heparanase (IC50 = 0.4 µM), an enzyme that cleaves heparan sulfate into glucuronic acid (GlcUA) and N-acetylglucosamine (GlcNAc). OGT 2115 also showed antiangiogenic properties (IC50=1 μM). |
| In vitro | OGT 2115 obviously inhibits the invasion and migration induced by Adriamycin. Furthermore, the MTT assay results display that OGT 2115 does not decrease the anti-proliferative effect of Adriamycin. Heparanase InhibitorOGT 2115 can inhibit metastasis induced by endoplasmic reticulum (ER) stress in breast cancer cells, although not significantly. The number and rate of migrated cells are significantly reduced following the exposure of the cells to Tunicamycin + OGT 2115, compared with the control group [2]. |
| In vivo | OGT 2115 displays a plasma concentration of ~10x the heparanase IC50 following oral dosing at 20 mg/kg when administered to mice[1]. |
| Target activity | Heparanase:0.4 μM |
| molecular weight | 495.3 |
| Molecular formula | C24H16BrFN2O4 |
| CAS | 853929-59-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 1 mg/ml, Sonication is recommended. |
| References | 1. Courtney SM, et al. Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor. Bioorg Med Chem Lett. 2005 May 2;15(9):2295-9. 2. Li Y, et al. Suppression of endoplasmic reticulum stress-induced invasion and migration of breast cancer cells through the downregulation of heparanase. Int J Mol Med. 2013 May;31(5):1234-42. |