UBA6-IN-1 is a UBA6/UBE1L2 inhibitor ( IC50 ≤50 nM) that acts by reducing the level of squalene epoxidase ( SQLE ). UBA6-IN-1 affects SREBP -dependent lipid metabolism processes and downstream cholesteryl ester transport, and can be used for cancer research [1].
In Vitro, UBA6-IN-1 (I-01) potently inhibits Uba6 enzyme activity, achieving 87% inhibition at 0.123 μM[1]. UBA6-IN-1 (10 μM; 6 h) alters SREBP-dependent lipid metabolism in WSU-DLCL2 cells when treated at 10 μM for 6 hours, as indicated by reduced SQLE protein levels[1].
References:
[1]. Benjamin S, et al. INDOLE-SUBSTITUTED PYRROLOPYRIMIDINYL INHIBITORS OF Uba6. WO2014022744A1. 2013-08-02.
In Vitro, UBA6-IN-1 (I-01) potently inhibits Uba6 enzyme activity, achieving 87% inhibition at 0.123 μM[1]. UBA6-IN-1 (10 μM; 6 h) alters SREBP-dependent lipid metabolism in WSU-DLCL2 cells when treated at 10 μM for 6 hours, as indicated by reduced SQLE protein levels[1].
References:
[1]. Benjamin S, et al. INDOLE-SUBSTITUTED PYRROLOPYRIMIDINYL INHIBITORS OF Uba6. WO2014022744A1. 2013-08-02.