2-D08

2-D08 is a synthetic flavone that inhibits sumoylation.¹ It completely inhibits sumoylation in microfluidic electrophoretic mobility shift and kinetic assays at a concentration of 30 µM. 2-D08 inhibits sumoylation of topoisomerase I in the breast cancer cell lines ZR-75-1 and BT-474.² It specifically disrupts the transfer of SUMO from the E2 enzyme (UBC9) thioester conjugate to the substrate. 2-D08 prevents amyloid-β (Aβ) (1-42) aggregation and Aβ-induced toxicity in PC12 cells.³ It also has antioxidant properties.⁴

WARNING This product is not for human or veterinary use.

1. Kim, Y.S., Keyser, S.G., and Schneekloth, J.S., Jr. Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation. Bioorg. Med. Chem. 24(4), 1094-1097 (2014).

2. Kim, Y.S., Nagy, K., Keyser, S., et al. An electrophoretic mobility shift assay identifies a mechanistically unique inhibitor of protein sumoylation. Chem. Biol. 20(4), 604-613 (2013).

3. Marsh, D.T., Das, S., Ridell, J., et al. Structure-activity relationships for flavone interactions with amyloid β reveal a novel anti-aggregatory and neuroprotective effect of 2',3',4'-trihydroxyflavone (2-D08). Bioorg. Med. Chem. 25(14), 3827-3834 (2017).

4. Cotelle, N., Bernier, J.L., Hénichart, J.P., et al. Scavenger and antioxidant properties of ten synthetic flavones. Free Radic. Biol. Med. 13(3), 211-219 (1992).