品牌	貨號	產品規格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S94740-5mg	97%	￥260.00元	6	-	-	-
源葉(MedMol)	S94740-10mg	97%	￥450.00元	7	-	-	-
源葉(MedMol)	S94740-25mg	97%	￥900.00元	6	-	-	-
源葉(MedMol)	S94740-50mg	97%	￥1530.00元	5	-	-	-
源葉(MedMol)	S94740-100mg	97%	￥2600.00元	5	-	-	-

產品介紹

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

產品描述： 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

靶點： SETD8/KMT5A;HistoneMethyltransferase

體外研究：
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.

體內研究：
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.

參考文獻：
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

保存條件： -20°C

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

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UNC0379 97%

6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine