GSK J4 HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GSK J4是一种有效的细胞通透性组蛋白H3赖氨酸27（H3K27）去甲基化酶JMJD3抑制剂，IC50值大于50 μM。JMJD3是调控转录染色质复合体的必要成分[1]。
GSK J4是GSK-J1的乙酯衍生物。GSK J1是一种有效的JMJD3抑制剂，IC50值为60 nM。由于强极性羧基的存在，GSK J4具有受限的细胞通透性，给药后快速被巨噬细胞酯酶水解，从而导致药理学相关的细胞内GSK-J1浓度的产生[1]。
据报道，GSK J4也剂量依赖地抑制肿瘤坏死因子α（TNF-α）的产生，IC50值为9 μM。TNF-α是参与各种炎症性疾病的LPS驱动的细胞因子。
参考文献：
[1] Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. doi: 10.1038/nature11262.
- 1. Silasi M, You Y, et al. "Human Chorionic Gonadotropin modulates CXCL10 Expression through Histone Methylation in human decidua." Sci Rep. 2020;10(1):5785. PMID:32238853
- 2. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 453.96 |
| Cas No. | 1797983-09-5 |
| Formula | C24H27N5O2·HCl |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥13.9 mg/mL in DMSO |
| Chemical Name | ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate |
| SDF | Download SDF |
| Canonical SMILES | CCOC(=O)CCNC1=NC(=NC(=C1)N2CCC3=CC=CC=C3CC2)C4=CC=CC=N4.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
人类原代巨噬细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
1、3、10和31 μM；6小时 |
|
实验结果 |
GSK J4呈剂量依赖性地抑制TNF-α蛋白产生，其IC50值为9 μM。 |
| 动物实验 [2]: | |
|
动物模型 |
携带SF8628 K27M异种移植瘤的小鼠模型 |
|
给药剂量 |
100 mg/kg/day；腹腔注射；持续10天 |
|
实验结果 |
GSK J4显著抑制SF8628皮下肿瘤生长。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. [2]. Hashizume R, Andor N, Ihara Y, Lerner R, Gan H, Chen X, Fang D, Huang X, Tom MW, Ngo V, Solomon D, Mueller S, Paris PL, Zhang Z, Petritsch C, Gupta N, Waldman TA, James CD. Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma. Nat Med. 2014 Dec;20(12):1394-6. |
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| 描述 | GSK J4 HCl是GSK-J1的乙酯衍生物。 | |||||
| 靶点 | JMJD3 | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
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