Fig. 1: BRD-810 is a potent and selective inhibitor of the antiapoptotic protein MCL1. | Nature Cancer

Fig. 1: BRD-810 is a potent and selective inhibitor of the antiapoptotic protein MCL1.

From: BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models

Fig. 1

a, The key compounds from the macrocyclic MCL1 inhibitor class. b, Overlay of BRD-810 (orange sticks) and modified Bim BH3 peptide SAH-MS1-18 (magenta cartoon, PDB 5W89) in the BH3 binding pocket. c,d, Quantification of the MCL1–BAK (c) or MCL1–BIM (d) complex, measuring the interaction between native cellular MCL1 protein and BAK or BIM using ELISA. Data are shown as the mean and s.d. (n = 3 independent measurements). e,f, Activation of caspases 3 and 7 (e) and cell viability (f) under increasing doses of BRD-810 in parental HMC1-8 cells, CRISPR-edited BAK;BAX-knockout cells and HMC1-8-Cas9-expressing control cells. Data are shown as the mean and s.d. (n = 2 independent measurements).

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