Table 1 Inhibitors used in the inhibitor screening assay.
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. |