IRE1α kinase-IN-1 NEW
| Price | $118 | $297 | $475 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: IRE1α kinase-IN-1 | CAS No.: 2328097-41-0 |
| Purity: 99.18% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | IRE1α kinase-IN-1 |
| 描述 | IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM). |
| 體外活性 | IRE1α kinase-IN-1 (compound 31) effectively mitigates endoplasmic reticulum stress by hindering IRE1α oligomerization and phosphorylation, while also suppressing its endoribonuclease activity within human cells[1]. This compound demonstrates high specificity, showing greater than 70% inhibition for only 4 out of 455 kinases tested, indicating its select focus on IRE1α. It attenuates recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM and disrupts ATP-site LanthaScreen tracer binding to the recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1]. Additionally, it prevents tunicamycin-induced GFP-IRE1α foci formation in HEK293 cells with an IC50 of 0.74 μM and obstructs both tunicamycin- and thapsigargin-induced IRE1α-dependent XBP1 mRNA splicing, with IC50 values ranging from 0.68 to 1.63 μM in the same cell line[1]. In H929 and NCI-H929 cells, IRE1α kinase-IN-1 dose-dependently suppresses IRE1α-dependent XBP1s mRNA expression when applied at concentrations between 0 to 20 μM, demonstrating its potent inhibitory activity on tunicamycin-induced XBP1s expression[1]. |
| 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 : 10 mg/mL (19.8 mM), Sonication is recommended. |
| 關(guān)鍵字 | endoribonuclease | Inositol requiring enzyme 1 | cells | IRE1a kinase-IN-1 | IRE1 | oligomerization | IRE-1α kinase-IN-1 | selectivity | IRE1α kinase IN 1 | Inhibitor | IRE1α kinase-IN-1 | inhibit | IRE1alpha kinase-IN-1 | HEK293 | autophosphorylation | reticulum | IRE1α kinaseIN1 | endoplasmic |
| 相關(guān)產(chǎn)品 | B I09 | Sunitinib | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | Sunitinib Malate | D-F07 | MKC8866 | APY29 | GSK2850163 (S enantiomer) | 4μ8C | GSK2850163 | Toyocamycin | IXA4 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 內(nèi)質(zhì)網(wǎng)應(yīng)激化合物庫 | 激酶抑制劑庫 | 抑制劑庫 | 已知活性化合物庫 | 抗癌化合物庫 |
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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