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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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