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KIRA6

产品编号: DC10542 Featured
KIRA6
结构式
1589527-65-0
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中国地区超过5000个高品质化合物库存
应用领域
KIRA6，小分子 IRE1α RNase 激酶抑制剂，IC50 值为0.6 µM。 KIRA6 可以触发细胞凋亡 (apoptotic) 反应。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1589527-65-0
名称: N-[4-[8-amino-3-(1,1-dimethylethyl)imidazo[1,5-a]pyrazin-1-yl]-1-naphthalenyl]-N'-[3-(trifluoromethyl)phenyl]-urea
别名: KIRA6,IRE1 Inhibitor IV,IRE1α Kinase Inhibiting RNase Attenuator 6
SMILES: NC1=NC=CN2C1=C(C3=C(C=CC=C4)C4=C(NC(NC5=CC(C(F)(F)F)=CC=C5)=O)C=C3)N=C2C(C)(C)C
分子式: C28H25F3N6O
分子量: 518.5
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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