UBA5-IN-1

UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme

IC50: 4.0 μM (UBA5), 78.5 μM (UAE), 66.8 μM (NAE)[1]

UBA5-IN-1 (0.1-1000 μM) shows dose-dependent inhibition effect to UBA5 with an IC50 value of 4.0 μM, and inhibits UAE and NAE with IC50 values of 78.5 and 66.8 μM, respectively[1]. UBA5-IN-1 (0-5 μM) inhibits UBA5 non-competitively with respect to ATP[1]. UBA5-IN-1 (10 μM) shows no effect on ATP binding to human kinase[1]. UBA5-IN-1 (0-50 μM; 72 h) effects cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1]. Cell Proliferation Assay[1] Cell Line: Sk-Luci6 cancer cells with high expression levels of UBA5 Concentration: 0-50 μM Incubation Time: 0-72 h Result: Showed selective anti-proliferative activity for Sk-Luci6 cancer cells which expressed higher UBA5 protein levels, but showed no anti-proliferative activity to MRC9 lung fibroblasts and A549 carcinoma cells.

[1]. da Silva SR, et al. A selective inhibitor of the UFM1-activating enzyme, UBA5. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4542-4547.