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AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM, without significant inhibition on 26 other kinases tested. AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein with IC50 of 2.7 μM, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway. In hippocampal slices, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide. While in NGP and SH-5Y-SY cells, AR-A014418 reduces neuroendocrine markers and suppresses neuroblastoma cell growth. AR-A 014418, 48 hrs posttreatment, caused dose (25-100 μ M) dependent inhibition in U373 and U87 cell viability with also inhibition in activating tyrosine phosphorylation of GSK3alpha (Tyr 279) and beta (Tyr 216).
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Source | Cell Death Dis (2018). Figure 5. AR-A014418 |
| Method | i.v. | |
| Cell Lines | seipin-nKO mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 28 days | |
| Results | As shown in Fig. 5b, the level of cleaved caspase-3 (c-caspase-3) in the SN of 8-M-old seipin-nKO mice was higher than that in control mice (P < 0.01, n =6), whereas there was no significant difference between 3-M-old control mice and seipin-nKO mice |
| Molecular Weight | 308.31 |
| Formula | C12H12N4O4S |
| CAS Number | 487021-52-3 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GSK-3 Products |
|---|
| CHIR-99021
CHIR-99021 (CT99021) is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. |
| CHIR-99021 HCl
CHIR-99021 HCl (Laduviglusib; CT99021) is a hydrochloride of CHIR-99021, with IC50 of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively. |
| SB 216763
SB 216763 is a potent and selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM for GSK-3α. |
| AZD2858
AZD2858 is a potent, orally bioactive inhibitor of GSK-3 with an IC50 of 68 nM. |
| Indirubin
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of ~75 nM and 0.19 μM. |
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