KIRA9
KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.
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- CAS 番号: 2922507-65-9
- 分子式: C27H27F3N6O3S
- 分子量:572.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
IC50: 4.8 μM (IRE1) in INS-1 cells[1]
体外実験
KIRA9 (0-30 μM; 2 hours) blocks the autophosphorylation induced by conditional overexpression of IRE1α in INS-1 cells (IC50=4.8 μM)[1].
KIRA9 (20 μM; 2 hours) reduces the mRNA expression of Bloc1s1, Ins1 and Ins2 in INS-1 cells[1].
KIRA9 (20 μM; 2 hours) blunts IRE1α-dependent decay (RIDD) in ER-stressed INS-1 cells[1].
KIRA9 (20 μM; 1 hour) markedly reduces the generation of cleaved caspase-3 and shows significant cytoprotective efficacy[1].
KIRA9 (0-20 μM; 3 days) reduces XBP1s expression, plasma cell differentiation and IgM secretion in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:INS-1 cells[1]
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Concentration:20 μM
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Incubation Time:1 hour
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Result:Markedly reduced the generation of cleaved caspase-3 and showed significant cytoprotective efficacy.
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Cell Line:Mouse splenocytes (LPS-treated)[1]
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Concentration:0, 1.25, 2.5, 5.0, 10 and 20 μM
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Incubation Time:3 days
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Result:Reduced XBP1s expression, plasma cell differentiation and IgM secretion in a dose-dependent manner.
化学情報
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CAS 番号 2922507-65-9
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分子量 572.60
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分子式 C27H27F3N6O3S
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SMILES
O=S(NC1=CC=C(OC2=NC=CC=C2C3=CC=NC(N[C@@H]4CNCCC4)=N3)C5=C1C=CC=C5)(CCC(F)(F)F)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)