产品说明书
MKC8866
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同义名 : | Orin1001;IRE1-IN-8866 |
| CAS号 : | 1338934-59-0 | |
| 货号 : | A1003533 | |
| 分子式 : | C18H19NO7 | |
| 纯度 : | 99%+ | |
| 分子量 : | 361.346 | |
| MDL号 : | MFCD31540824 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 5 mg/mL(13.84 mM)，配合低频超声，并水浴加热至45℃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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Cells operate a signaling network termed the unfolded protein response (UPR) to monitor protein-folding capacity in the endoplasmic reticulum (ER). Inositol-requiring enzyme 1 (IRE1) is an ER transmembrane sensor that activates the UPR to maintain the ER and cellular function. Although mammalian IRE1 promotes cell survival, it can initiate apoptosis via decay of antiapoptotic miRNAs[2]. MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits DTT-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstressed RPMI 8226 cells with an IC50 of 0.14 μM[3]. MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells and MKC8866 (20 μM; 72 hours) is sufficient to completely block paclitaxel-induced expression of XBP1s[3]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth[4]. In female athymic nude mice with MDA-MB-231 tumor, MKC8866 (oral 300 mg/kg for 28 days) reduced tumor regrowth post-paclitaxel withdrawal[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.84mL 2.77mL 1.38mL |
27.67mL 5.53mL 2.77mL |
| 参考文献 |
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