KIRA6
货号:
19151-1mg 基本售价:
406.0 元 规格:
1 mg
产品信息
概述货号 | 19151-1mg |
描述 | The IRE1 pathway is a component of the unfolded protein response that senses unfolded proteins via an ER luminal domain that becomes oligomerized during stress. It is associated with promoting cell survival through the activity of the IRE1α RNase, whose activity upregulates proteins that enhance ER protein folding and quality control. However, under high ER stress, the IRE1α RNase becomes hyperactive and is less discriminant in its substrate specificity, endonucleolytically cleaving many additional mRNAs that localize to the ER membrane, leading to cell proliferation blocks, inflammation, and apoptosis. KIRA6 is an ATP-competitive IRE1α kinase inhibiting RNase attenuator (KIRA) that allosterically inhibits IRE1α RNase kinase activity (IC50 = 0.6 µM) and prevents oligomerization.1 It has been shown to inhibit IRE1α in vivo and to promote cell survival under ER stress.1 At 20 µg/ml, KIRA6 is reported to preserve photoreceptor functional viability in rat models of ER stress-induced retinal degeneration.1 At 5 mg/kg, it has also been shown to preserve pancreatic β cells, increase insulin, and reduce hyperglycemia in Akita diabetic mice.2 |
别名 | IRE1 Inhibitor IV;IRE1α Kinase Inhibiting RNase Attenuator 6; |
性能供应商 | Cayman |
应用文献 |
1.Ghosh, R.,Likun, W.,Wang, E.S., et al. Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress. Cell 158(3), 534-548 (2014). 2.Cosgrove, S.B.,Wren, J.A.,Cleaver, D.M., et al. Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet.Dermatol. 24(5), (2013).
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运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 518.5 |
分子式 | C28H25F3N6O |
CAS号 | 1589527-65-0 |
稳定性 | ≥ 2 years |
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