Table 1 Inhibitors used in the inhibitor screening assay.

From: Development of a novel immunoassay to detect interactions with the transactivation domain of p53: application to screening of new drugs

Inhibitor

Structure

MW/Formula/CAS No.

Description

Nutlin-3a

581.49 C30H30Cl2N4O4 4675576-98-4

The active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.

Idasanutlin

616.48 C31H29Cl2F2N3O4 1229705-06-9

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM.

YH239-EE

504.41 C25H27Cl2N3O4 1364488-67-4

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

MI-773

562.50 C29H34Cl2FN3O3 1303607-60-4

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

NVP-CGM097

659.26 C38H47ClN4O4 1313363-54-0

NVP-CGM097 is a highly potent and selective MDM2 inhibitor, disrupting the interaction between both proteins.

RG-7112

726.28 C38H48Cl2N4O4S 939981-39-2

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor. Phase 1.