Product Details
| Product Name:
GSK2606414 |
CAS No.:
1337531-36-8 |
| Purity:
98.44% |
Supply Ability:
10g |
| Release date:
2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | GSK2606414 |
| 描述 | GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase（PERK）inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice. |
| 體外活性 | METHODS: S1-M1-80 vector and S1-M1-80 sgABCG2 cells were treated with GSK2606414 (0.1, 1, 3, 10, 30, 100 μM, 72 hours), and cytotoxicity was determined by MTT assay.
RESULTS GSK2606414 showed dose-dependent cytotoxic effects on both cell lines. [2]
METHODS: N2A cells were treated with GSK2606414 (0.5, 1 μM, 24 hours) and high glucose (30 mM), cells were lysed, and Western blot analysis was performed.
RESULTS N2A cells treated with GSK2606414 reduced the phosphorylation of eIF2α in cells and significantly reduced p-PERK levels in a dose-dependent manner, and GSK2606414 could inhibit the PERK/p-eIF2α/ATF4/CHOP signaling axis. [3] |
| 體內(nèi)活性 | METHODS: GSK2606414 (50, 150 mg/kg, oral, twice a day, 21 days) was used to treat mice bearing subcutaneous pancreatic human BxPC3 tumors and the effect on tumor growth was observed.
RESULTS GSK2606414 inhibited tumor growth in a dose-dependent manner, with the tumor growth inhibition rates of 20% and 59% at the two doses, respectively. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (110.76 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Inhibitor | GSK-2606414 | Apoptosis | Autophagy | PKR-like endoplasmic reticulum kinase | GSK2606414 | GSK 2606414 | inhibit | PERK | Protein kinase R-like endoplasmic reticulum kinase |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 成骨分子庫(kù) | 經(jīng)典已知活性庫(kù) | 內(nèi)質(zhì)網(wǎng)應(yīng)激化合物庫(kù) | 激酶抑制劑庫(kù) | 自噬庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 含氟化合物庫(kù) |
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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
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$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States