TH34 是一种 HDAC6/8/10 抑制剂,IC50 分别为 4.6 μM、1.9 μM 和 7.7 μM,对 HDAC1/2/3 具有高选择性。
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TH34 is a potent HDAC6/8/10 inhibitor. TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines. The combination of TH34 with plasma-achievable concentrations of retinoic acid, a drug applied in neuroblastoma therapy, synergistically inhibits colony growth (combination index (CI) 0.1 for 10 μM of each). In summary, our study supports using selective HDAC inhibitors as targeted antineoplastic agents and underlines the therapeutic potential of selective HDAC6/8/10 inhibition in high-grade neuroblastoma.
Reference
[1].Kolbinger FR, Koeneke E, Ridinger J, Heimburg T, Müller M, Bayer T, Sippl W,?Jung M, Gunkel N, Miller AK, Westermann F, Witt O, Oehme I. The HDAC6/8/10?inhibitor TH34 induces DNA damage-mediated cell death in human high-grade?neuroblastoma cell lines. Arch Toxicol. 2018 Aug;92(8):2649-2664. doi:?10.1007/s00204-018-2234-8. Epub 2018 Jun 9. PubMed PMID: 29947893; PubMed Central?
PMCID: PMC6063332.
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