An article HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells WOS:000585952100044 published article about HISTONE DEACETYLASE INHIBITOR; DRUG-COMBINATION; CERVICAL-CANCER; ACTIVATION; OLIGOMERIZATION; CHEMOTHERAPY; CHIDAMIDE; SYNERGY; BREAST; DEATH in [Liang, Tao; Zhou, Yi; Elhassan, Reham M.; Hou, Xuben; Yang, Xinying; Fang, Hao] Shandong Univ, Cheeloo Coll Med, Sch Pharmaceut Sci, Key Lab Chem Biol,Minist Educ,Dept Med Chem, Jinan 250012, Shandong, Peoples R China in 2020.0, Cited 40.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4. SDS of cas: 99-93-4
Inspired by the synergistic effect of BTSA1 (a Bax activator) and SAHA (a histone deacetylase (HDAC) inhibitor) in HeLa cell growth suppression, a series of novel HDAC-Bax multiple ligands were designed rationally. Compound 23, which possesses similar HDAC inhibitory activity relative to SAHA and Bax affinity comparable to BTSA1, exhibits a superior growth suppression against HeLa cells, and its antiproliferative activities are 15-fold and 3-fold higher than BTSA1 and SAHA, respectively. The better antiproliferative activity and lower cytotoxicity of compound 23 indicated that our HDAC-Bax multiple ligand design strategy achieved success. Further studies suggested that compound 23 could enhance Bax-dependent apoptosis by upregulating Bax, followed by inducing the conformational activation of Bax. To our knowledge, we first report HDAC-Bax multiple ligands and demonstrate a new paradigm for the treatment of solid tumors by enhancing Bax-dependent apoptosis.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles