Bioactivity | Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562)[1]. |
CAS | 3059615-90-3 |
Formula | C24H25N3O5 |
Molar Mass | 435.47 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Wang B, et al. Indolo[3,2-c]isoquinoline Hydroxamic Acid Derivatives as Novel Orally Topoisomerase-Histone Deacetylase Dual Inhibitors for NSCLC Therapy. J Med Chem. 2024 Oct 23. |