• 产品描述： UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma

• 靶点： SETD8/KMT5A;HistoneMethyltransferase

• 体外研究：
  UNC0379 (1-10 μM, 9 days) inhibits HGSOC cells proliferation. UNC0379 (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells. UNC0379 (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation Cell Viability Assay Cell Line: JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu Concentration: 1-10 μM Incubation Time: 9 days Result: Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 µM. Cell Cycle Analysis Cell Line: JHOS3, OVCAR3 Concentration: 10 µM Incubation Time: 96 h Result: Arrested cells in sub-G1 phase.

• 体内研究：
  UNC0379 (intratracheal administration, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse. Animal Model: Bleomycin (BLM)-induced lung fibrosis mouse model Dosage: 1 mg/kg/day Administration: Intratracheal administration, on day7, 8, and 9. Result: Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.

• 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. 3. Keita Ugai, et al. Inhibition of the SET8 Pathway Ameliorates Lung Fibrosis Even Through Fibroblast Dedifferentiation. Front Mol Biosci. 2020 Aug 5;7:192.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.418 ml	12.09 ml	24.181 ml
  5 mM	0.484 ml	2.418 ml	4.836 ml
  10 mM	0.242 ml	1.209 ml	2.418 ml
  50 mM	0.048 ml	0.242 ml	0.484 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *