规格

价格

库存

数量

2 mg

¥ 397

现货

5 mg

¥ 617

现货

10 mg

¥ 956

现货

25 mg

¥ 1,840

现货

50 mg

¥ 2,996

现货

100 mg

¥ 3,770

现货

200 mg

¥ 5,420

现货

1 mL x 10 mM (in DMSO)

¥ 683

现货

生物活性

产品描述	GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
靶点活性	JMJD3:
体外活性	方法: 前列腺癌症细胞系 R1-AD1、R1-D567、R1-I567、CWR22Rv-1 和 PC3 用 GSK-J4 (0-32 µM) 处理 72 h，通过 Alamar blue reagent 检测细胞活力。结果: GSK-J4 对 PC 细胞具有细胞生长抑制和/或细胞毒性作用。CWR22Rv-1 对治疗最敏感，ED50 约为 3 µM。[1] 方法: 人急性髓系白血病细胞 KG-1a 用 GSK-J4 (2-10 µM) 处理 48 h，通过 Flow cytometry 检测细胞凋亡。结果: GSK-J4 治疗组 KG-1a 细胞的凋亡率与对照组相比显著增加。[2]
体内活性	方法: 为研究对败血症的作用，将 GSK-J4 (1-3 mg/kg) 腹腔注射给 ICR 小鼠，1 h 后注射细菌悬液诱导败血症。结果: GSKJ4 对 JMJD3 的药理学抑制保护小鼠免受早期败血症死亡，并减少促炎细胞因子 IL-1β 的产生以及 IL-6、TNF-α 和 MCP-1 的表达。[3]
动物实验	GSK-J4 is prepared in DMSO and diluted 1/10 with ethanol.Six-to eight-week-old female C57BL/6 WT mice are injected by subcutaneous injection (s.c.) with 50 μg myelin oligodendrocyte glycoprotein 35-55 peptide (pMOG) emulsified in Complete Freund's Adjuvant (CFA) supplemented with heat-inactivated Mycobacterium tuberculosis H37 RA. In addition, mice receive intraperitoneal injection (i.p.) of 500 ng of pertussis toxin on days 0 and 2. Clinical signs are assessed daily according to the following scoring criteria: 0, no detectable signs; 1, flaccid tail; 2, hind limb weakness or abnormal gait; 3, complete hind limb paralysis; 4, paralysis of fore and hind limbs; and 5, moribund or death. A stock solution of GSK-J4 of 42 mg/mL (100 mM) is prepared in dimethyl sulfoxide (DMSO) to preserve stability. Before injection, the stock solution is diluted 1/10 with ethanol (DMSO: ethanol, 1:10 v/v) and brought to a final concentration of 140 μg/mL in PBS. In systemic drug evaluation experiments, each mouse receive daily i.p. injections (from days 0-5) of 100 μL of this solution containing 14.0 μg of the GSK-J4 (equivalent to 0.56 mg/kg of the drug). Control mice receive 100 μL of the vehicle during the same period. In other EAE experiments, 106 bone marrow-derived DCs from WT mice are treated with GSK-J4 or vehicle alone for 16 h, pulsed with 5 μg/mL of pMOG for 4 h and then transferred i.v. into WT C57BL/6 recipient mice 14 and 7 days before EAE induction. In other adoptive transfer EAE experiments, CD4+Foxp3+ Treg cells generated in the presence or absence of 25 nM GSK-J4 are purified by cell sorting and then 0.75×106 transferred i.v. into WT C57BL/6 recipient mice 1 day before EAE induction.
别名	GSK J4

化学信息

分子量	417.5
分子式	C₂₄H₂₇N₅O₂
CAS No.	1373423-53-0
Smiles	CCOC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
密度	1.216 g/cm3 (Predicted)

储存&溶解度

存储

溶解度信息

Ethanol: 41.75 mg/mL (100 mM), Sonication is recommended.

DMSO: 141 mg/mL (337.72 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.18 mg/mL (10.01 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3952 mL	11.9760 mL	23.9521 mL	119.7605 mL
5 mM	0.4790 mL	2.3952 mL	4.7904 mL	23.9521 mL
10 mM	0.2395 mL	1.1976 mL	2.3952 mL	11.9760 mL
20 mM	0.1198 mL	0.5988 mL	1.1976 mL	5.9880 mL
50 mM	0.0479 mL	0.2395 mL	0.4790 mL	2.3952 mL
100 mM	0.0240 mL	0.1198 mL	0.2395 mL	1.1976 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

GSK-J4

GSK-J4

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

GSK-J4

GSK-J4

GSK-J4 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词