nutlin 1

Nutlin-1 is a p53-MDM2 binding inhibitor, p-Glycoprotein (p-gp) transport substrate, and antitumor agent.

Nutlin-C1-amido-PEG4-C2-N3 is a novel ligand-linker conjugate for the E3 ligase, incorporating the MDM2 ligand from Nutlin 3 and a 4-unit PEG linker. This compound is specifically designed for use in PROTAC technology.

Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 positions on two of the phenyl rings rather than a single 4-chloro as seen in nutlin-3. At high concentrations, caylin-1 inhibits the growth of HCT116 cells with an IC50 value of approximately 7 μM, making it about 7-fold less potent than nutlin-3 in the same assay. Interestingly, at concentrations at or below 1 μM, caylin-1 promotes the growth of HCT116 cells approximately 20% compared to untreated cells. The mechanism of the growth promoting properties of caylin-1 have not yet been elucidated.

Nutlin-3b ((+)-Nutlin-3) is a p53 MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

Nutlin Carboxylic Acid (MDM2 ligand 1), derived from Nutlin 3, serves as an MDM2 ligand. It can be attached to a protein ligand via a linker to create PROTACs[1].

(4R,5S)-Nutlin Carboxylic Acid (MDM2 Ligand 2), a Nutlin 3-based MDM2 ligand, can be conjugated to a protein-binding ligand via a linker to create PROTACs[1].