AR-A014418
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥493.00 | 现货 | |
| 5mg | ￥331.00 | 现货 | |
| 10mg | ￥531.00 | 现货 | |
| 50mg | ￥1433.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
AR-A014418是一种选择性的GSK-3抑制剂。
糖原合酶激酶-3（GSK3）是一种丝氨酸/苏氨酸激酶，与病理情况，如糖尿病和阿尔茨海默病（AD）相关。
体外实验：ARA014418以ATP竞争性的方式起作用，不能显著抑制cdk2、cdk5或26种其它激酶，表明其对GSK3的高特异性。在稳定表达人四重复tau蛋白的细胞中，ARA014418抑制GSK3对tau蛋白特异性位点（Ser-396）的磷酸化[1]。
体内实验：ARA014418可引起行为改变，其与抗抑郁药物的效应是一致的。在公认的用于检测抗抑郁效应的大鼠强迫游泳实验中，AR-A014418亚急性腹腔注射后减少不动时间。而且，AR-A014418还可减少自发及苯丙胺诱导的活性，支持了该效应的特异性[2]。
参考文献：
[1] Bhat R, Xue Y, Berg S, Hellberg S, Orm? M, Nilsson Y, Rades?ter AC, Jerning E, Markgren PO, Borgeg?rd T, Nyl?f M, Giménez-Cassina A, Hernández F, Lucas JJ, Díaz-Nido J, Avila J. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003;278(46):45937-45.
[2] Gould TD, Einat H, Bhat R, Manji HK. AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int J Neuropsychopharmacol. 2004;7(4):387-90.
产品性质
| 物理外观 | A solid |
| CAS号 | 487021-52-3 |
| 分子式 | C12H12N4O4S |
| 分子量 | 308.31 |
| 化学名称 | 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea |
| 溶解度 | insoluble in EtOH; insoluble in H2O; ≥15.4 mg/mL in DMSO |
| SMILES | COc1ccc(CNC(Nc2ncc([N+]([O-])=O)[s]2)=O)cc1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | AR-A014418是一种ATP竞争性的和选择性的GSK3β抑制剂，IC50和Ki值分别为104 nM和38 nM。 |
| 靶点 | GSK-3 |
| 生物活性数据 | 104 +/- 27 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 9 篇科研文献
- 1. Jing-Ting Chiou, Chia-Chi Hsu, et al. "Cytarabine-induced destabilization of MCL1 mRNA and protein triggers apoptosis in leukemia cells." Biochem Pharmacol. 2023 May:211:115494. PMID: 36924905
- 2. Sergey V. Rozhkov, Kristina A. Sharlo, et al. "The Role of Glycogen Synthase Kinase-3 in the Regulation of Ribosome Biogenesis in Rat Soleus Muscle under Disuse Conditions." Int J Mol Sci. 2022 Mar 2;23(5):2751. PMID:35269893
- 3. Jing‐Ting Chiou, Nan‐Chieh Huang, et al. "NOXA-mediated degradation of MCL1 and BCL2L1 causes apoptosis of daunorubicin-treated human acute myeloid leukemia cells." J Cell Physiol. 2021 Nov;236(11):7356-7375. PMID:33982799
- 4. Qiang Li, Dongmei Yu, et al. "TIPE3 promotes non-small cell lung cancer progression via the protein kinase B/extracellular signal-regulated kinase 1/2-glycogen synthase kinase 3β-β-catenin/Snail axis." Transl Lung Cancer Res. 2021 Feb;10(2):936-954. PMID:33718034
- 5. Binyan Lin, Yongxu Li, et al. "CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK." Oncogene. 2020 Sep;39(37):6024-6040. PMID:32778769
- 6. Lee YC, Shi YJ, et al. "GSK3β suppression inhibits MCL1 protein synthesis in human acute myeloid leukemia cells." J Cell Physiol. 2020;10.1002/jcp.29884. PMID:32572959
- 7. Huang CH, Lee YC, et al. "Arsenic trioxide-induced p38 MAPK and Akt mediated MCL1 downregulation causes apoptosis of BCR-ABL1-positive leukemia cells." Toxicol Appl Pharmacol. 2020;397:115013. PMID:32305283
- 8. Chen YJ, Huang CH, et al. "The suppressive effect of arsenic trioxide on TET2-FOXP3-Lyn-Akt axis-modulated MCL1 expression induces apoptosis in human leukemia cells." Toxicol Appl Pharmacol. 2018 Nov 1;358:43-55. PMID:30213730
- 9. Lee YC, Chen YJ, et al. "Amsacrine-induced apoptosis of human leukemia U937 cells is mediated by the inhibition of AKT- and ERK-induced stabilization of MCL1." Apoptosis. 2016 Oct 19. PMID:27757735
沪公网安备 31011002003500