p53-y220c

p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2 p53), which induces apoptosis.

MB710 is an amino benzothiazole derivative that binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro. It exhibits anticancer activity and can be used in cancer research.

PhiKan 083 hydrochloride, a carbazole derivative, binds to the surface cavity and stabilizes Y220C (Kd: 167 μM) with a relative binding affinity (Kd) of 150 μM in Ln229 cells.

PhiKan 083, a carbazole derivative, exhibits potential as an eco-friendly dye with applications in the development of organic photovoltaic cells (OPVs).

MS182 (compound 11), an acetylation targeting chimera (AceTAC), incorporates p53 Y220C stabilizers with p300 CBP binders, connected via a linker. This design enables MS182 to selectively form a ternary complex with p300 CBP acetyltransferase and the mutant p53 Y220C, subsequently catalyzing specific acetylation of lysine at position 382 in a time- and concentration-dependent manner, achieving an ACE 50 of 1.52 μM. Additionally, MS182 demonstrated significant bioavailability in mice, with GI 50 values recorded at 2.16 μM for BxPC3 (p53 Y220C -) and 1.83 μM for NUGC (p53 Y220C +).

MB725 is a strong and selective inducer of viability reduction in several cancer cell lines containing the oncogenic p53-Y220C mutation.

The protein p53, often called the 'guardian of the genome,' is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. PK7242 is an inducer of reactivation of mutant p53 in cancer cells. In cancer cells carrying the Y220C mutant, PK7242 binds to the p53-Y220C core domain and induces growth inhibition, cell-cycle arrest, and apoptosis.

SLMP53-2 is a mutant p53 reactivator that restores the wild-type-like conformation and DNA-binding ability of mutp53-Y220C through enhanced interaction with Hsp70, thereby reinstating p53's transcriptional activity. This compound induces cell cycle arrest, apoptosis, and endoplasmic reticulum (ER) stress, displaying antitumor activity [1] [2].

Rezatapopt (PC14586) is a small molecule p53 reactivator with anti-tumor activity that selectively binds to the cleft present in the TP53 Y220C mutant protein and restores the p53 wild-type (normal) conformation and transcriptional activity, and can be used to study locally advanced or metastatic solid tumors.

P53 Activator 11 (compound A-1) is a highly effective p53 activator, demonstrating an EC50 value of 0.478 µM for p53 (Y220C). It holds potential for cancer research [1].