Table 1 Amino acid sequence and their respective IC50s (competition assay) of stapled peptides synthesised by Brown et al. and Chang et al. used in this study.

From: Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays

Peptide

Amino acid sequence

Mdm2 IC 50 (μM)

Mdm4 IC 50 (μM)

Staplin-Control

Ac-1TSAXrEYAALAXs11-NH2

>10

>10

Staplin

Ac-1TSFXrEYWALLXs11-NH2

0.94 ± 0.0410

0.66 ± 0.0610

Staplin-2

Ac-1TSFXrEYW(6Cl)WALLXs11-NH2

0.32 ± 0.0210

3.49 ± 0.6310

ATSP-7041

Ac-1LTFXrEYWAQ(Cba)XSSAA14-NH2

0.9111

2.3111

Nutlin-3a

N.A.

0.096

>106

  1. Nutlin-3 was used as a positive control for Mdm2 thermal stabilisation. IC50s are obtained from the references indicated.
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