
KIRA6
CAS No. 1589527-65-0
KIRA6 ( —— )
产品货号. M22059 CAS No. 1589527-65-0
KIRA6 是 IRE1α RNase 激酶的有效抑制剂 (IC50: 0.6 μM)。它可以触发细胞凋亡反应。KIRA6(10-1000 nM,72 小时)在低 nM 浓度下强烈损害 KIT 依赖性细胞系 HMC-1.1 的活力,其方式与 KIT 阻断一致。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥437 | 有现货 |
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5MG | ¥737 | 有现货 |
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10MG | ¥1134 | 有现货 |
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25MG | ¥2317 | 有现货 |
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50MG | ¥3345 | 有现货 |
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100MG | ¥4982 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称KIRA6
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述KIRA6 是 IRE1α RNase 激酶的有效抑制剂 (IC50: 0.6 μM)。它可以触发细胞凋亡反应。KIRA6(10-1000 nM,72 小时)在低 nM 浓度下强烈损害 KIT 依赖性细胞系 HMC-1.1 的活力,其方式与 KIT 阻断一致。
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产品描述KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.KIRA6 (10-1000 nM, 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade. KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 ?μM. KIRA6 (10-1000 nM, 1 hour) reduces signaling output of KIT, including the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2.KIRA6 (1 μM, 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation in a dose-dependent manner. KIRA6 (0.1-10μM, 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner [2].KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to the vehicle, both fed ad lib. KIRA6 (i.p, 5 mg/kg, 21 or 18 days post injections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at a high level after stopping injections in the Akita Mouse.
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体外实验Cell Viability Assay Cell Line:HMC-1.1 cellsConcentration:10 nM, 30 nM, 100 nM, 300 nM, 1000 nM Incubation Time:72 hours Result:Inhibited cell viability from 30 nM.Western Blot Analysis Cell Line:HMC-1.1 cells Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1000 nM Incubation Time:1 hours Result:Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.RT-PCRCell Line:INS-1 IRE1α (WT) cells Concentration:1 μM Incubation Time: 0 hour, 12 hours, 24 hours, 48 hours Result:Inhibited Ins1 mRNA expression.Apoptosis Analysis Cell Line:INS-1 IRE1α (WT) cells Concentration:1-10 μM Incubation Time:72 hours Result:Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.
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体内实验Animal Model:Male Ins2+/Akita miceDosage:5 mg/kg Administration:Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections Result:Attenuates b cell functional loss, increased insulin levels.
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同义词——
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通路Others
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靶点Other Targets
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受体IRE1α
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研究领域——
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适应症——
化学信息
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CAS Number1589527-65-0
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分子量518.53
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分子式C28H25F3N6O
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纯度>98% (HPLC)
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溶解度DMSO:5 mg/mL (9.64 mM);Ethanol:2 mg/mL (3.86 mM; Need ultrasonic)
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SMILESCC(C)(C)C1=NC(=C2N1C=CN=C2N)C1=CC=C(NC(=O)NC2=CC=CC(=C2)C(F)(F)F)C2=CC=CC=C12
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Mahameed M,et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis. 2019 Apr 1;10(4):300.
产品手册




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