UNC0379
CAS No. 1620401-82-2
UNC0379 ( UNC 0379 | UNC-0379 )
产品货号. M12379 CAS No. 1620401-82-2
UNC0379 是赖氨酸甲基转移酶 SETD8 的选择性底物竞争性抑制剂,IC50 为 7.3 uM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ¥381 | 有现货 |
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| 10MG | ¥648 | 有现货 |
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| 25MG | ¥1183 | 有现货 |
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| 50MG | ¥2001 | 有现货 |
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| 100MG | ¥3013 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称UNC0379
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述UNC0379 是赖氨酸甲基转移酶 SETD8 的选择性底物竞争性抑制剂,IC50 为 7.3 uM。
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产品描述UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 with IC50 of 7.3 uM, displays good selectivity over 15 other methyltransferases, including G9a and GLP (IC50>100 uM); causes neuroblastoma (NB) cell growth inhibition which is p53 dependent, reduces levels of p53K382me1 modification in xenografts.
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体外实验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 hResult:Arrested cells in sub-G1 phase.
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体内实验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 modelDosage: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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同义词UNC 0379 | UNC-0379
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通路Chromatin/Epigenetic
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靶点HMTase
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受体SETD8
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研究领域Other Indications
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适应症——
化学信息
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CAS Number1620401-82-2
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分子量413.5563
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分子式C23H35N5O2
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCOC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1
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化学全称4-Quinazolinamine, 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Ma A, et al. J Med Chem. 2014 Aug 14;57(15):6822-33.
2. Ma A, et al. Medchemcomm. 2014 Dec;5(12):1892-1898.
3. Veschi V, et al. Cancer Cell. 2017 Jan 9;31(1):50-63.
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