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IRE1α kinase-IN-1 Sale

目录号 : GC63513

IRE1α kinase-IN-1 是一种高度选择性的 IRE1α (ERN1) 抑制剂,IC50 为 77 nM。IRE1α kinase-IN-1 对 IRE1α 的选择性比 IRE1β 亚型高 100 倍。IRE1α kinase-IN-1 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)。

IRE1α kinase-IN-1 Chemical Structure

Cas No.:2328097-41-0

规格 价格 库存 购买数量
5 mg
¥4,050.00
现货
10 mg
¥7,200.00
现货
25 mg
¥14,850.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)[1].

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].

[1]. Colombano G, et al. Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease. J Med Chem. 2019;62(5):2447-2465.

Chemical Properties

Cas No. 2328097-41-0 SDF
分子式 C26H26ClFN8 分子量 504.99
溶解度 DMSO : 25 mg/mL (49.51 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9802 mL 9.9012 mL 19.8024 mL
5 mM 0.396 mL 1.9802 mL 3.9605 mL
10 mM 0.198 mL 0.9901 mL 1.9802 mL
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