p53

p53 and MDM2 proteins-interaction-inhibitor racemic is an inhibitor of the interaction between p53 and MDM2 proteins.

MI-1061 TFA is a potent inhibitor of the MDM2-p53 interaction, exhibiting an IC50 of 4.4 nM and a Ki of 0.16 nM. This orally bioavailable and chemically stable compound effectively activates p53, leading to apoptosis in SJSA-1 xenograft tumor tissues in murine models. MI-1061 TFA demonstrates significant anti-tumor activity, making it a valuable tool for cancer research focused on the modulation of the p53 signaling pathway.

DS-5272 is an orally active inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 20 nM. This compound effectively inhibits the proliferation of SJSA-1 cells (wildtype p53, IC50 = 0.17 μM) as well as DLD-1 cells (mutant p53). DS-5272 induces cell cycle arrest and promotes apoptosis in SJSA-1 cells, while also exhibiting antitumor efficacy in vivo in mouse models. This makes DS-5272 a valuable tool for research in cancer therapeutics targeting the p53 pathway.

p53-MDM2-IN-6 is a selective inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 11.08 µg/mL. This compound effectively induces cell cycle arrest in the S phase and promotes both early and late apoptosis in HT29 colorectal cancer cell lines, with an IC50 of 10.44 µg/mL. Its ability to elevate p53 levels while decreasing GST enzyme expression highlights its potential as a valuable tool for investigating therapeutic strategies in colorectal cancer research.

p53-MDM2-IN-5 is a potent inhibitor of the p53-MDM2 interaction. This compound induces apoptosis, promotes autophagy, and causes DNA damage in cells, contributing to its anti-tumor efficacy. Additionally, p53-MDM2-IN-5 effectively induces cell cycle arrest at both the S and G2/M phases, making it a valuable tool for cancer research applications focused on therapeutic strategies targeting the p53 pathway.

MI-773 TFA is a selective inhibitor of the MDM2-p53 interaction, demonstrating a Ki of 0.88 nM for MDM2. By disrupting the MDM2-TP53 interaction, MI-773 TFA effectively activates the p53 tumor suppressor pathway, leading to apoptotic cell death. This compound has shown significant anticancer activity, inducing tumor regression in xenograft models of adenoid cystic carcinoma and exhibiting therapeutic potential in neuroblastoma. MI-773 TFA serves as a valuable tool for research focused on p53-related cancer therapies.

YL-1-9 is a potent inhibitor of p53 degradation mediated by MDM2, achieved through its strong binding to critical hydrophobic pockets within the MDM2 protein. This compound effectively induces cell cycle arrest and promotes apoptosis, particularly in breast cancer cells. YL-1-9 is valuable for research into p53-targeted therapies and the mechanisms of cancer cell proliferation and survival.

NSC194598 is a p53 DNA-binding inhibitor that effectively disrupts the interaction between p53 and DNA, exhibiting an IC50 value of 180 nM for in vitro studies and a range of 2-40 μM for in vivo applications. This compound has been shown to interfere with the transcriptional activation of the mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 is utilized in research investigating acute toxicity effects on normal tissues due to radiation and chemotherapy.