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GSK-J4 hydrochloride
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品牌名称:$brandModel.Title(进口品牌)型号:_Histone Demethylase 原产地:中国大陆 发布时间:2020/7/15更新时间:2024/1/2
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GSK-J4 hydrochloride
CAS No. : 1797983-09-5
MCE 站:GSK-J4 hydrochloride
产品活性:GSK-J4 hydrochloride 是一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂,IC50 分别为 8.6 μM 和 6.6 μM。GSK-J4 hydrochloride 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α,IC50 值为 9 μM。GSK-J4 hydrochloride 是 GSK-J1 的细胞通透性前药。
研究领域:Epigenetics
作用靶点:Histone Demethylase
In Vitro: GSK-J4 Hydrochloride 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 Hydrochloride (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 Hydrochloride (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 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1.
GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.
In Vivo: GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.
GSK-J4 Hydrochloride (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.
相关产品:Anti-Cancer Compound Library | Epigenetics Compound Library | Bioactive Compound Library Plus | Histone Modification Research Compound Library | Diabetes Related Compound Library | GSK-J4 | QC6352 | SP2509 | ORY-1001(trans) | GSK2879552 | CPI-455 | GSK-LSD1 dihydrochloride | Seclidemstat | Tranylcypromine hemisulfate | Corin | JIB-04 | IOX1 | NCGC00244536 | KDM5-IN-1 | AS8351 | Daminozide | KDM5A-IN-1 | KDM4D-IN-1 | ML324 | KDOAM-25 citrate | NCGC00247743 | L-2-Hydroxyglutaric acid disodium | PBIT | Procaine | T-3775440 hydrochloride | T-448 | GSK 690 Hydrochloride | GSK467 | OG-L002
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