GCN2iB NEW
| Price | $77 | $178 | $288 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: GCN2iB | CAS No.: 2183470-12-2 |
| Purity: 99.08% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | GCN2iB |
| 描述 | GCN2iB is an ATP-competitive inhibitor of serine/threonine protein kinase, stress-responsive kinase (GCN2), with IC50 of 2.4 nM. |
| 體外活性 | 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] |
| 體內(nèi)活性 | 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] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (121.73 mM), Sonication is recommended. H2O : < 0.1 mg/mL (insoluble) |
| 關(guān)鍵字 | inhibit | GCN-2iB | Inhibitor | Eukaryotic Initiation Factor (eIF) | Autophagy | GCN2iB |
| 相關(guān)產(chǎn)品 | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 自噬庫 | 抑制劑庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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