UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC 50 of 7.3 μM, K D value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
性状
Solid
IC50 & Target[1][2]
SETD8 (KMT5A)
体外研究(In Vitro)
UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation.UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells.UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686.
溶解度数据
In Vitro: H2O : 100 mg/mL (189.54 mM; Need ultrasonic)配制储备液
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686.