| CAS NO: | 1630086-20-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| Cas No. | 1630086-20-2 |
| 别名 | AMG-18 |
| Canonical SMILES | O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(OC4=NC=CC=C4C5=NC(N[C@@H]6CNCCC6)=NC=C5)C3=CC=C2)=O |
| 分子式 | C31H29ClN6O3S |
| 分子量 | 601.12 |
| 溶解度 | DMSO : 65 mg/mL (108.13 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α's RNase[1]. Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2[1]. Kira8 efficaciously reverses established diabetes in non-obese diabetic (NOD) mice by sparing β-cells and preserving their physiological function. Kira8 is first tested in 3-week-old male pre-diabetic Akita mice by i.p. daily dosing of 50 mg/kg, whereupon significant reduction of hyperglycemia becomes apparent over several weeks. Then Kira8 (50 mg/kg) is tested in the complex NOD. Showing target engagement, one week treatment of pre-diabetic NODs with Kira8 leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserved Ins1/Ins2, BiP and MANF mRNAs[1]. [1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8. |
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