Stemcell, 100-1559, CUDC-101

Elicit anti-tumor activity in a variety of cancer types with CUDC-101, a potent inhibitor of class I and II histone deacetylases (HDACs; IC50 = 4.5 - 13.5 nM), epidermal growth factor receptor (EGFR, also known as HER1; IC50 = 2.4 nM), and human epidermal growth factor receptor 2 (HER2; IC50 = 16.4 nM) in cancer cells (Lai et al. Cancer Res, 2010). By integrating multiple inhibitory functional groups, CUDC-101 can simultaneously inhibit HDACs substrate bonding and compete with ATP binding to function as an EGFR and HER2 inhibitor (Cai et al. J Med Chem, 2010). HDAC inhibitors have been associated with immune response modulation by regulating expression of molecules that impact antigen presentation and immune cell activation (Banik et al. Int J Mol Sci, 2019).

CUDC-101 has been used for:

CANCER RESEARCH

· Inhibit cell proliferation, promote cell death, reduce cell migration in human anaplastic thyroid cancer cell lines, and inhibit tumor growth in a mouse model (Zhang et al. Oncotarget, 2015).

· Reduce tumor growth in mouse and human breast tumor organoids and enhance tumor antigen presentation in breast cancer cells (Zhou et al. Nat Biomed Eng, 2021).

· Induce cell cycle arrest and cell death in human multiple myeloma cells and reduce tumor size in a mouse xenograft model (Cao et al. J Zhejiang Univ Sci B, 2023).