Fig. 2: Keap1 PINCHs precipitate Keap1 in cells.
From: A pharmacological modality to sequester homomeric proteins
a, Chemical structures of Keap1-targeting PINCHs. EC50 values for the active compounds are shown in parentheses. b, WB of EL229’s effect on Keap1 in the soluble and insoluble phases of OCI-AML2 cells (20 h of treatment). Representative results from two independent experiments are shown. c, WB of EL133’s effect on soluble Keap1 in OCI-AML2 (20 h of treatment). Representative results from two independent experiments are shown. d, EL133 affects Keap1 in the soluble and insoluble OCI-AML2 cell phases, in a time-dependent and dose-dependent manner. WB band quantification from three independent experiments and EC50 curves for individual compounds are shown in Supplementary Fig. 3b. UT, untreated. e, Global proteomics analysis of the soluble lysate of U2OS cells, showing significant downregulation of Keap1 following treatment with EL133 (250 nM, 20 h) compared to an equivalent amount of BDX (500 nM). The dotted lines mark a twofold reduction in protein level (vertical) and P = 0.05 significance in a double-sided Student’s t-test (horizontal).
