Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM),对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化,并抑制 IRE1α RNase 活性 (IC50=80 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,480 | 现货 | ||
5 mg | ¥ 3,630 | 现货 | ||
10 mg | ¥ 5,230 | 现货 | ||
25 mg | ¥ 8,150 | 现货 | ||
50 mg | ¥ 10,900 | 现货 | ||
100 mg | ¥ 14,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,090 | 现货 |
产品描述 | IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) |
体外活性 |
IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells[1]. IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1]. IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM[1]. IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells[1]. |
分子量 | 504.99 |
分子式 | C26H26ClFN8 |
CAS No. | 2328097-41-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (19.8 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9802 mL | 9.9012 mL | 19.8024 mL | 49.5059 mL |
5 mM | 0.396 mL | 1.9802 mL | 3.9605 mL | 9.9012 mL | |
10 mM | 0.198 mL | 0.9901 mL | 1.9802 mL | 4.9506 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
IRE1α kinase-IN-1 2328097-41-0 Cell Cycle/Checkpoint IRE1 endoribonuclease Inositol requiring enzyme 1 cells IRE1a kinase-IN-1 oligomerization IRE-1α kinase-IN-1 selectivity IRE1α kinase IN 1 Inhibitor inhibit IRE1alpha kinase-IN-1 HEK293 autophosphorylation reticulum IRE1α kinaseIN1 endoplasmic inhibitor