Recent studies have uncovered the potential of dual LSD1-HDAC inhibitors (tranylcypromine-based hydroxamic acids) as a promising therapy for colorectal cancer (CRC). Among these, Compound 2 has demonstrated impressive anti-cancer activity, suppressing the growth of CRC cells (GI50 = 0.495 μM in HCT-116 cells) while significantly reducing colony formation and inducing cell cycle arrest.

Building on these promising results, we offer a collection of over 1,300 analogs (in-stock and make-on-demand) based on Compound 2. We believe there is significant potential to design even more potent and selective inhibitors as perspective drugs for CRC treatment.

At the molecular level, Compound 2 preferentially inhibits HDAC6, alongside potent LSD1 inhibition, upregulating epigenetic markers. Importantly, it has also demonstrated robust in vivo antitumor efficacy in xenograft mouse models and patient-derived CRC organoids, outperforming standard-of-care irinotecan.

We invite collaboration to further study this promising compound class. For orders and inquiries, please contact us at sales@chem-space.com.