| Name | GCN2iB |
| Description | GCN2iB is an ATP-competitive inhibitor of serine/threonine protein kinase, stress-responsive kinase (GCN2), with IC50 of 2.4 nM. |
| In vitro | METHODS: HEK293 cells were treated with 4 nM to 4 μM Gcn2iB for 6 h in the presence or absence of Halofuginone (HF) treatment to explore the concentration-dependent effect of Gcn2iB on ISR activation.
RESULTS HF treatment resulted in increased levels of p-Gcn2, p-eIF2α, and Atf4, each of which decreased with increasing concentrations of Gcn2iB; p-Gcn2 induction decreased at 62.5 nM Gcn2iB or higher, and Atf4 induction decreased at 250 nM Gcn2iB; cells treated with Gcn2iB in the absence of HF exhibited a biphasic response to the induction of p-Gcn2, p-eIF2α, and Atf4, with increases in all three ISR markers observed in the range of 10 to 100 nM Gcn2iB; above 250 nM Gcn2iB, p-Gcn2 levels decreased to below those determined with vehicle, and Atf4 levels were not significantly induced; although Gcn2iB could inhibit Gcn2 stimulation by HF treatment, lower concentrations of Gcn2iB activated Gcn2 and the ISR in the absence of external stress. [1] |
| In vivo | METHODS: HFD plus STZ-induced diabetic C57BL/6J mice were treated with intraperitoneal injection of GCN2iB (3 mg/kg) every other day for 6 weeks. At the end of the experiment, the mice were subjected to echocardiography.
RESULTS After GCN2iB treatment, the fasting blood glucose level (11.18 ± 1.44 vs. 17.42 ± 2.57 mmol/L) and body weight (28.94 ± 2.05 vs. 32.54 ± 1.49 g) of type 2 diabetic mice were significantly reduced; GCN2iB treatment had no effect on heart weight. Significant effects, but increased heart weight to body weight ratio; GCN2iB treatment significantly improved cardiac systolic function and increased left ventricular (LV) ejection fraction (EF). [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (121.73 mM), Sonication is recommended.
H2O : < 0.1 mg/mL (insoluble)
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| Keywords | inhibit | GCN-2iB | Inhibitor | Eukaryotic Initiation Factor (eIF) | Autophagy | GCN2iB |
| Inhibitors Related | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
