Skip to main content
. Author manuscript; available in PMC: 2021 Apr 17.
Published in final edited form as: ACS Chem Biol. 2020 Mar 19;15(4):895–903. doi: 10.1021/acschembio.0c00124

Figure 2.

Figure 2.

Mechanism of ligand-dependent luminescence at physiological temperature. (a) Cycloheximide-enabled determination of ENL(YEATS)-HiBiT half-life when treated with vehicle or drug. The depicted HiBiT luminescence measures of protein abundance are normalized to pre-treatment levels (N = 3, mean ± s.e.m.). (b) Kinetics of ENL(YEATS)-HiBiT luminescence after SGC-iMLLT treatment with values normalized to 24-hour DMSO treatment (N = 10, mean ± s.e.m.). (c) Schematic depiction of HiBiT CETSA performed on pre-lysed cells. (d) Raw luminescence values for HiBiT CETSA performed on cell lysates treated with vehicle or SGC-iMLLT (N = 4, mean ± s.e.m.). (e) CETSA melt curve of SMARCA4(bromodomain)-HiBiT in OCI/AML-2 cells after 1-hour treatments with drug or vehicle (N = 3, mean ± s.e.m.). (f) CETSA melt curve for ENL(YEATS)-HiBiT performed by treating cell lysates with a peptide substrate, H3K27cr (N = 3, mean ± s.e.m.).