S81303 |
GSK-J1 |
源叶(MedMol) | 99% |
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- 产品描述: GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
- 靶点: IC50: 60 nM (KDM6B);HistoneDemethylase
- 体外研究:
GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively
- 参考文献:
1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. 2. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2 3. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.568 ml 12.839 ml 25.677 ml 5 mM 0.514 ml 2.568 ml 5.135 ml 10 mM 0.257 ml 1.284 ml 2.568 ml 50 mM 0.051 ml 0.257 ml 0.514 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)