1,7-Heptanediol serves as a PROTAC linker for connecting E3 ubiquitin ligase ligands and target protein ligands[1-2]. 1,7-Heptanediol can be used in pharmaceutical intermediates, disease treatment, and PROTAC technology research[3-4].
In vitro, 1,7-Heptanediol (20mg/mL) was used to treat CT26, 4T1, SMMC-7721, and NCI-H1299 cells for 1 hour, 1,7-Heptanediol exhibited significant cytotoxicity against 4T1 cells. Treatment of 4T1 cells with 1,7-Heptanediol (1–5mg/mL) for 24 hours showed marked toxicity. 4T1 cells were treated with 1,7-Heptanediol liposomes (with a lipid concentration of 4 µg/mL) for 24 hours. 1,7-Heptanediol caused a decrease in mitochondrial membrane potential and promoted cell apoptosis. After a 12-hour treatment, 1,7-Heptanediol significantly increased ATP levels in the cell supernatant and induced immunogenic cell death[5].
References:
[1] De Paoli G, Bell S. A rapid GC-MS determination of gamma-hydroxybutyrate in saliva. J Anal Toxicol. 2008 May;32(4):298-302.
[2] Paborji M, Waugh WN, Stella VJ. Mechanistic investigation of the degradation of sulfamic acid 1,7-heptanediyl ester, an experimental cytotoxic agent, in water and 18oxygen-enriched water. J Pharm Sci. 1987 Feb;76(2):161-5.
[3] Özeren HD, Capezza AJ, Gharbi S, et al. Starch/Alkane Diol Materials: Unexpected Ultraporous Surfaces, Near-Isoporous Cores, and Films Moving on Water. ACS Omega. 2020 Oct 30;5(44):28863-28869
[4] Vinogradov SV, Suzdaltseva Y, Alakhov VYu, et al. Inhibition of herpes simplex virus 1 reproduction with hydrophobized antisense oligonucleotides. Biochem Biophys Res Commun. 1994 Sep 15;203(2):959-66.
[5] Gu M, Yu W, Stefanello ST, et al. Synergistic in vivo anticancer effects of 1,7-heptanediol and doxorubicin co-loadedliposomes in highly aggressive breast cancer. J Control Release. 2025 Jan 10;377:174-185.