MYC-IN-4 is a MYC inhibitor that disrupts the interaction between MYC/MAX proteins with an IC50 of 3.06 μM. It inhibits MYC-aberrant PC-3 prostate cancer cells, exhibiting an IC50 of 0.440 μM. In FVB mice with Myc-CaP prostate tumor xenografts, MYC-IN-4 demonstrates significant antitumor efficacy. This compound is useful for prostate cancer research.

MYC-IN-4 (Compound 15) exhibits potent antiproliferative activity against PC-3 cells (MYC aberrant prostate cancer cells) with an IC 50 value of 0.440 μM. It demonstrates broad-spectrum antiproliferative effects across 14 other tumor cell lines, such as MDA-MB-231, HCT-116, Myc-CaP, LN-CaP, NCI-H1581, A549, SK-N-BE, SK-OV-3, HepG-2, A-204, A-431, MG-63, LP-1, and MV4-11, with IC 50 values ranging from 0.331 μM to 2.60 μM. In PC-3 cells, MYC-IN-4 (10 μM, 1 h) significantly disrupts MYC/MAX protein-protein interactions (PPI) as shown by Co-IP experiments. Additionally, in a cell-free AlphaLISA assay, MYC-IN-4 (0.1-100 μM, 2 h) inhibits MYC/MAX PPI with an IC 50 of 3.06 μM. It also reduces the thermal stability of endogenous MYC in PC-3 cells at 10 μM for 1 hour. MYC-IN-4 induces concentration-dependent MYC degradation within the PC-3 cell line at concentrations of 1-10 μM over 24 hours. Furthermore, it inhibits MYC transcriptional activity in HEK293T cells transfected with an E-box luciferase reporter plasmid, with an IC 50 of 0.739 μM.

MYC-IN-4 (Compound 15), administered intraperitoneally at doses of 10-50 mg/kg every other day for 16 days, demonstrated significant antitumor efficacy in FVB mice with Myc-CaP prostate tumor xenografts.