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AR-A014418 AR 0133418; GSK 3β inhibitor VIII; AR 014418

AR-A014418 是一种有效,选择性,ATP 竞争性的 GSK3β 抑制剂 (IC50=104 nM; Ki=38 nM)。

  • 货号:
    TK0411
  • 规格:
    5mg
    10mg
    50mg
  • 价格:
    0.00

产品参数

CAS No.487021-52-3
生物活性AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM).
分子式C12H12N4O4S
分子量308.31
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder -20°C 3 years
溶解性数据DMSO : ≥ 100 mg/mL (324.35 mM)
体内研究AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, enhances motor activity, blocks disease progression, and postpons the endpoint of the disease in ALS mouse model with the G93A mutant human SOD1. Furthermore, AR-A014418 suppresses acetic acid- and formalin-induced nociception in mice via modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord.
体外研究AR-A014418 blocks the phosphorylation of tau at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein, with an IC50 of 2.7 μM, and protects cultured N2A cells from death cuased by PI3K/PKB pathway blockage. AR-A014418 also shows inhibitory effect on neurodegeneration mediated by beta-amyloid peptide in hippocampal slices. AR-A014418 decreases neuroendocrine markers and suppresses neuroblastoma cell growth in NGP and SH-5Y-SY cells.
文献•J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. •Cell Syst. 2018 Apr 25;6(4):424-443.e7. •J Cell Physiol. 2019 Jul;234(7):10411-10420. •FASEB J. 2020 Jan;34(1):1481-1496. •Toxicol Sci. 2018 Apr 1;162(2):475-487. •Toxicol Appl Pharmacol. 2020 Apr 17;397:115013.
纯度及产品资料98%