nutlin-1

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

(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].

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].

Nutlin-C1-amido-PEG4-C2-N3 is a novel compound that functions as a ligand-linker conjugate for the E3 ligase. It is a synthesized molecule incorporating the MDM2 ligand derived from Nutlin 3, and a 4-unit PEG linker. This compound is specifically designed for utilization 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) 是一种 p53 MDM2 拮抗剂或抑制剂，IC50为 13.6 μM。它与 MDM2 的结合活性比 Nutlin-3a 低 150 倍。