MYCi975

MYCi975 is a potent, selective, orally active small molecule inhibitor of MYC (also known as c-Myc), a transcription factor that regulates cell growth, metabolism, apoptosis, and is a validated driver of oncogenesis in multiple tumor types. MYCi975 acts by binding directly to MYC, inhibiting its function and promoting its degradation through enhancement of GSK-3β-mediated phosphorylation, leading to selective inhibition of MYC target gene expression and increased cancer cell apoptosis. The agent demonstrates anti-proliferative effects, induces apoptosis, overcomes resistance to multiple chemotherapies (e.g., cisplatin), eliminates cancer stem cells, prevents metastasis, and activates intrinsic immune responses (including enhanced immune cell infiltration and upregulation of PD-L1 expression). MYCi975 is efficacious in vitro against breast cancer—including triple-negative breast cancer (TNBC), head and neck squamous cell carcinoma (HNSCC), prostate cancer, hepatocellular carcinoma, and multiple myeloma. Preclinically, it shows synergy with established agents such as doxorubicin, paclitaxel, and anti-PD1 therapy, and demonstrates greater tolerability compared to earlier MYC inhibitors. It was initially developed by Shenzhen ICarbonX Living Healthcare Management.