中文名称: GSK-J4 hydrochloride
英文名称: GSK-J4 hydrochloride
CAS No: 1797983-09-5
分子式: C24H28ClN5O2
分子量: 453.96
G10426 GSK-J4 hydrochloride ≥98% (psaitong)
包装规格:
100mg in glass bottle
溶解性:
溶于DMSO(62.5mg/mL 超声)
产品描述:

基本信息

产品编号:G10426

产品名称:GSK-J4 hydrochloride

CAS:

1797983-09-5

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C24H28ClN5O2

溶于液体

-80℃

六个月

分子量:

453.96

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

90mg/mL warmed with 50ºC water bath (198.25mM)

Ethanol

90mg/mL warmed with 50ºC water bath (198.25mM)

Water

10mg/mL (22.02mM)

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.2028mL

11.0142mL

22.0284mL

5mM

0.4406mL

2.2028mL

4.4057mL

10mM

0.2203mL

1.1014mL

2.2028mL

50mM

0.0441mL

0.2203mL

0.4406mL

 

生物活性

产品描述

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 8.6μM 和 6.6μM。GSK-J4 hydrochloride 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α,IC50 值为 9μM。GSK-J4 hydrochloride 是 GSK-J1 的细胞通透性前药。

靶点/IC50

JMJD3
(Cell-free assay)

60nM

 

体外研究

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 (5μM;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 (10,25nM) 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.

体内研究

GSK-J4 Hydrochloride (10mg/kg;i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.GSK-J4 Hydrochloride (0.5mg/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 on a BKS background

Dosage:

10mg/kg

Administration:

i.p.;thrice-weekly for 10 weeks

Result:

Attenuated the development of kidney disease in diabetic mice.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):