貨號	規格	價格	上海	北京	武漢	南京
S80305-1mg	98.4%	￥323.00 S80305-1mg ￥323.00 現貨	8 8	-	-	-
S80305-5mg	98.4%	￥450.00 S80305-5mg ￥450.00 現貨	7 7	-	-	-
S80305-10mg	98.4%	￥720.00 S80305-10mg ￥720.00 現貨	3 3	-	-	-
S80305-25mg	≥98%	￥1440.00 S80305-25mg ￥1440.00 2-3天	0 貨期：2-3天	-	-	-
S80305-50mg	≥98%	￥2000.00 S80305-50mg ￥2000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis

產品描述：

靶點：

KDM6;HistoneDemethylase

體外研究：

GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α). GSK-J4 (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels. GSK-J4 (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells. GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1. GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells

體內研究：

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice. GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis. Animal Model: Eight-week-old male db/m and db/db mice Dosage: 10 mg/kg Administration: i.p.; thrice-weekly for 10 weeks Result: Attenuated the development of kidney disease in diabetic mice.

參考文獻：

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. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. 3. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117. 4. Xuan Chu, et al. GSK-J4 induces cell cycle arrest and apoptosis via ER stress and the synergism between GSK-J4 and decitabine in acute myeloid leukemia KG-1a cells. Cancer Cell International volume 20, Article number: 209 (2020). 5. Yapp C, et al. H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis. Arthritis Res Ther. 2016 Jul 7;18(1):158 6. Kamikawa YF, et al. Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cells. PLoS One. 2015 May 20;10(5):e0125626 7. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.395 ml	11.976 ml	23.952 ml
5 mM	0.479 ml	2.395 ml	4.79 ml
10 mM	0.24 ml	1.198 ml	2.395 ml
50 mM	0.048 ml	0.24 ml	0.479 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。

參考文獻

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