MDM-2/p53 Ligand

MDM2 ligand 5 is a Ligand for E3 Ligase that can be used for the synthesis of PROTACs.

PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53^Y220C-PLK1 ternary complex (EC₅₀ = 1.4 μM). PMV6-PEG4-BI2536 causes PLK1 mislocalization and inhibits PLK1 activity, inducing G2/M phase arrest and apoptosis in p53^Y220C-mutant cells, while sparing cells with wild-type TP53. PMV6-PEG4-BI2536 can be used in research on uterine, gastric, pancreatic, prostate, and breast cancers harboring the p53^Y220C mutation. PMV6-PEG4-BI2536 is composed of PMV6 (a p53^Y220C mutant-binding ligand), PEG4 (a linker), and BI2536 (HY-159493) (a PLK inhibitor).

SEN205A is a fragment compound that binds to the hydrophobic pocket of human S100B (K_d=0.5-1.0 mM), which is the key region for the interaction of S100B with TRTK-12 and p53, and SEN205A can be displaced from this site by TRTK-12. SEN205A exhibits excellent in vitro ADME properties, including high metabolic stability, chemical stability, and good solubility under physiological pH conditions. SEN205A can serve as a starting fragment for structure-based optimization to develop inhibitors targeting the S100B-p53 protein-protein interaction and investigate the pathogenesis of malignant melanoma.

SPDI-48-T1 is a lysine-stapled peptide. SPDI-48-T1 exhibits discernible binding affinities for MDM2 and MDMX, with K_d values of 396 nM and 456 nM, respectively. SPDI-48-T1 exhibits anticancer activity against breast cancer, colorectal cancer, non-small cell lung cancer, cervical cancer, and malignant melanoma.

p53 Y220C ligand-1(compound PK-A) is a target protein ligand of p53 DUBTAC modulator-1 (HY-180618). p53 Y220C ligand-1 exhibits potent activity in inhibiting cell proliferation in Huh7 cells.

MDM2 ligand 4 is the ligand for MDM2 that can be used for synthesis of PROTAC degrader KT-253 (HY-170451).

Rezatapopt analog-2 (compound A-15) is an analog of Rezatapopt (HY-156633) and can bind to P53.