Inhibitors of Lysine-specific Demethylases (LSDs)

LSD (lysine specific demethylase) is an enzyme which uses FAD (flavin adenine dinucleotide) as a coenzyme to demethylate methylated lysine in histone proteins. LSD has two isoforms (LSD1, LSD2). LSD1 is expected to be a therapeutic target for cancer, while LSD2 has numerous unknown functions and is currently under research to elucidate its function.^1-3) LSD Inhibitor S1024 (1) and LSD Inhibitor S1025 (2) exhibit equally potent inhibitory activity against LSD1 and different inhibitory activity against LSD2. 1 is also known to increase intracellular histone-modified H3K4me2 through its inhibitory effect.⁴⁾ In addition, 1 and 2 can be used for the research to elucidate the function of LSD2 taking advantage of the gap of their activity.

Related Products

B6490

LSD Inhibitor S1024

B6491

LSD Inhibitor S1025

P2908

trans-2-Phenylcyclopropanamine Hydrochloride

References

• 1) LSD1/KDM1A, a Gate-Keeper of Cancer Stemness and a Promising Therapeutic Target
  • P. Karakaidos, J. Verigos, A. Magklara, Cancers 2019, 11, 1821.
• 2) Overexpression of the shortest isoform of histone demethylase LSD1 primes hematopoietic stem cells for malignant transformation.
  • T. Wada, D. Koyama, J. Kikuchi, H. Honda, Y. Furukawa, Blood 2015, 125, 3731.
• 3) Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases
  • H. Niwa, T. Umehara, Epigenetics 2017, 12, 340.
• 4) Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2
  • H. Niwa, C. Watanabe, S. Sato, T. Harada, H. Watanabe, R. Tabusa, S. Fukasawa, A. Shiobara, T. Hashimoto, O. Ohno, K. Nakamura, K. Tsuganezawa, A. Tanaka, M. Shirouzu, T. Honma, K. Matsuno, T. Umehara, ACS Med. Chem. Lett. 2022, 13, 1485.

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