AR-A014418

SKU: orb1307275

Description

AR-A014418

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 487021-52-3
• MW: 308.31
• Purity: 100.00%
• Formula: C₁₂H₁₂N₄O₄S
• SMILES: COc1ccc(CNC(=O)Nc2ncc(s2)[N+]([O-])=O)cc1
• Target: GSK-3
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.49 mM);Ethanol:1.5 mg/mL (4.87 mM);DMSO:30.8 mg/mL (99.9 mM)

Bioactivity

• Target IC50:
  GSK-3β:38 nM(Ki)
• In Vivo:
  AR-A014418 inhibited neuroendocrine markers and inhibited the growth of neuroma cells in NGP cells and SH-5Y-SY cells.AR-A014418 inhibited neurodegeneration induced by β-like amyloid peptide in hippocampal slices.AR-A014418 inhibited the expression of tau in 3T3 fibroblasts expressing human four-repeat tau proteins at the GSK3-specific locus (Ser AR-A014418 inhibited tau phosphorylation at the GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human tetra-repeat tau protein with an IC50 of 2.7 μM and protected cultured N2A cells from death induced by blocking the PI3K/PKB pathway.
• In Vitro:
  AR-A014418 inhibited neuroendocrine markers and inhibited the growth of neuroma cells in NGP cells and SH-5Y-SY cells.AR-A014418 inhibited neurodegeneration induced by β-like amyloid peptide in hippocampal slices.AR-A014418 inhibited the expression of tau in 3T3 fibroblasts expressing human four-repeat tau proteins at the GSK3-specific locus (Ser AR-A014418 inhibited tau phosphorylation at the GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human tetra-repeat tau protein with an IC50 of 2.7 μM and protected cultured N2A cells from death induced by blocking the PI3K/PKB pathway.
• Cell Research:
  Cell viability is assessed by calcein/propidium iodide uptake. Calcein AM is taken up and cleaved by esterases present within living cells, yielding yellowish-green fluorescence, whereas PI is only taken up by dead cells, which become orange-red fluorescent. In brief, N2A cells are cultured for 2 days in vitro and then treated with 50 μM LY-294002 in the presence of AR-A014418 or vehicle (DMSO) for 24 h. Subsequently, N2A cells are incubated for 30 min with 2 μM PI and 1 μM calcein-AM. The cultures are then rinsed three times with Hanks' buffered saline solution containing 2 mM CaCl2, and the cells are visualized by fluorescence microscopy using a Zeiss Axiovert 135 microscope. Three fields (selected at random) are analyzed per well (∼300 cells/field) in at least three different experiments. Cell death is expressed as percentage of PI-positive cells from the total number of cells. In every experiment, specific cell death is obtained after subtracting the number of dead cells present in vehicle-treated cultures. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AR 0133418, AR 014418, AR-A 014418, ARA014418, AR-A014418, AR-A-014418, AR A014418, AR0133418, AR-0133418, AR014418, AR-014418, Glycogen synthase kinase-3, Glycogen synthase kinase 3, GSK3, GSK-3, GSK 3b inhibitor VIII, GSK 3beta inhibitor VIII, GSK 3β inhibitor VIII, GSK-3β, GSK-3beta Inhibitor VIII, GSK-3b Inhibitor VIII, GSK-3β Inhibitor VIII, inhibit, Inhibitor

Compound Identifiers

PubChem CID

448014