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CAS No. : 1797983-09-5
MCE 国际站: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 的细胞通透性前体。
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:Bioactive Compound Library Plus | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Anti-diabetic Compound Library | Anti-Cancer Metabolism Compound Library | Human Metabolite Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | GSK2879552 dihydrochloride | KDM2B-IN-3 | KDM4-IN-2 | LSD1/ER-IN-1 | Bomedemstat hydrochloride | LSD1-IN-18 | KDM4-IN-4 | (1S,2R)-Tranylcypromine hydrochloride | Pulrodemstat benzenesulfonate | GSK-J1 lithium salt | CPI-4203 | JQKD82 | Corin | Tranylcypromine hemisulfate | KDM2B-IN-4 | (1R,2S)-NCD38 TFA | LSD1-IN-14 | LSD1-IN-26 | Helenalin acetate | KDM2B-IN-2 | JHDM-IN-1 | Seclidemstat | KDM5-IN-1 | GSK-LSD1 dihydrochloride | LSD1-IN-21 | Arborinine | KDM4-IN-3
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