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编 号:F194257
分子式:C25H36F3N5O4
分子量:527.58
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生物活性:
UNC0379 TFA 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 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.

体内研究:
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.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.

体外研究:
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.
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