KIRA9 是一种有效的IRE1抑制剂 (INS-1 细胞中IC50=4.8 μM)。KIRA9 能够完全结合IRE1的 ATP 结合位点，可阻断内质网 (ER) 定位的 mRNA 衰减和细胞凋亡 (apoptosis)。
| 生物活性 | KIRA9 is a potentIRE1inhibitor (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 andapoptosis[1]. |
| IC50& Target | IC50: 4.8 μM (IRE1) in INS-1 cells[1] |
体外研究
(In Vitro) | 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].
Apoptosis Analysis | Cell Line: | INS-1 cells[1] | | Concentration: | 20 μM | | Incubation Time: | 1 hour | | Result: | Markedly reduced the generation of cleaved caspase-3 and showed significant cytoprotective efficacy. |
Cell Differentiation Assay | Cell Line: | Mouse splenocytes (LPS-treated)[1] | | Concentration: | 0, 1.25, 2.5, 5.0, 10 and 20 μM | | Incubation Time: | 3 days | | Result: | Reduced XBP1s expression, plasma cell differentiation and IgM secretion in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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