UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶SETD8(KMT5A) 抑制剂,IC50值为 7.3 μM,KD值 of 18.3 μM。UNC0379 TFA 可用于炎症癌症的研究,如肺纤维化,卵巢癌,神经母细胞瘤。
生物活性 | UNC0379 TFA is a selective, substrate-competitive inhibitor oflysine methyltransferase SETD8(KMT5A) with anIC50of 7.3 μM,KDvalue of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovariancancer, neuroblastoma[1][2][3]. |
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体外研究 (In Vitro) | UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2]. UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2]. UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation[3].
Cell Viability Assay[1] Cell Line: | JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu | Concentration: | 1-10 μM | Incubation Time: | 9 days | Result: | Inhibited HGSOC cells proliferation withIC50s ranging from 0.39 to 3.20 μM. |
Cell Cycle Analysis[1] Cell Line: | JHOS3, OVCAR3 | Concentration: | 10 μM | Incubation Time: | 96 h | Result: | Arrested cells in sub-G1 phase. |
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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[3].
Animal Model: | Bleomycin (BLM)-induced lung fibrosis mouse model[3] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(189.54 mM;Need ultrasonic) 配制储备液 1 mM | 1.8954 mL | 9.4772 mL | 18.9545 mL | 5 mM | 0.3791 mL | 1.8954 mL | 3.7909 mL | 10 mM | 0.1895 mL | 0.9477 mL | 1.8954 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |