Kira8
产品说明书
 |
同义名 : | AMG-18 |
| CAS号 : | 1630086-20-2 | |
| 货号 : | A649394 | |
| 分子式 : | C31H29ClN6O3S | |
| 纯度 : | 99%+ | |
| 分子量 : | 601.118 | |
| MDL号 : | MFCD28404657 | |
| 存储条件： |
Pure form Keep in dark place,Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 65 mg/mL(108.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 30 mg/mL(49.91 mM)，配合低频超声，水浴加热至45℃，并调节pH至2 无水乙醇: 75 mg/mL(124.77 mM)，配合低频超声，并调节pH至5，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | IRE1 (inositol requiring enzyme 1) is an ER transmembrane sensor that activates UPR to maintain ER and cellular function. It can promotes cell survive and initiate apoptosis via decay of anti-apoptotic microRNAs[1]. KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) that attenuates IRE1α endonuclease activity (IRE1α/β IC50 = 5/55 nM) with good kinome selectivity[2]. 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. Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks. One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs [3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.66mL 0.33mL 0.17mL |
8.32mL 1.66mL 0.83mL |
16.64mL 3.33mL 1.66mL |
| 参考文献 |
|---|