GSK-J4 NEW
| Price | $51 | $83 | $131 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-05 |
Product Details
| Product Name: GSK-J4 | CAS No.: 1373423-53-0 |
| Purity: 99.98% | Supply Ability: 10g |
| Release date: 2024/11/05 |
Product Introduction
Bioactivity
| 名稱 | GSK-J4 |
| 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. |
| 動物實驗 | 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. |
| 體外活性 | METHODS: Prostate cancer cell lines R1-AD1, R1-D567, R1-I567, CWR22Rv-1 and PC3 were treated with GSK-J4 (0-32 μM) for 72 h. Cell viability was measured by Alamar blue reagent. RESULTS: GSK-J4 had cell growth inhibitory and/or cytotoxic effects on PC cells. cWR22Rv-1 was the most sensitive to the treatment, with an ED50 of about 3 μM.[1] METHODS: Human acute myeloid leukemia cells KG-1a were treated with GSK-J4 (2-10 μM) for 48 h. Apoptosis was detected by Flow cytometry. RESULTS: The apoptosis rate of KG-1a cells in the GSK-J4 treatment group was significantly increased compared with the control group. [2] |
| 體內(nèi)活性 | METHODS: To investigate the effect on sepsis, GSK-J4 (1-3 mg/kg) was administered intraperitoneally to ICR mice, and sepsis was induced by injection of bacterial suspension 1 h later. RESULTS: Pharmacological inhibition of JMJD3 by GSKJ4 protected mice from early septic death and reduced the production of the pro-inflammatory cytokine IL-1β and the expression of IL-6, TNF-α and MCP-1. [3] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 41.75 mg/mL (100 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.18 mg/mL (10.01 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 60 mg/mL (143.71 mM) |
| 關(guān)鍵字 | GSKJ4 | Inhibitor | Apoptosis | H3K27me3/me2 | demethylase | diabetic | inflammation | Th17 | TGF-β | mice | cells | GSK-J4 | dendritic | GSK-J-4 | Histone Demethylase | inhibit | Th1 | GSK J4 |
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| 相關(guān)庫 | 細胞凋亡化合物庫 | 組蛋白修飾化合物庫 | 甲基化化合物庫 | 經(jīng)典已知活性庫 | 內(nèi)質(zhì)網(wǎng)應(yīng)激化合物庫 | 表觀遺傳庫 | 染色質(zhì)修飾分子庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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