STF-083010
产品说明书
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同义名 : | IRE1 Inhibitor I |
| CAS号 : | 307543-71-1 | |
| 货号 : | A276858 | |
| 分子式 : | C15H11NO3S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 317.383 | |
| MDL号 : | MFCD02332975 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(330.83 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 |
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| 动物实验配方： |
2% DMSO+40%PEG 300+5% Tween80 +water 2 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 描述 | STF-083010 is a novel Ire1 inhibitor which can Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. STF-083010 at 60μM inhibited endogenous XBP1 mRNA splicing in RPMI 8226 cells treated with 300nM thapsigargin. It inhibited the production of sXBP1 protein, but not the autophosphorylation of Ire1α, at 60μM in MM1.S and RPMI 8226 cell lines treated with 300nM thapsigargin. STF-083010 at 60mg/kg blocked bortezomib (1mg/kg)-induced XBP1 activity in vivo. Administration of STF-083010 at 30mg/kg, i.p., once weekly for 2 weeks, decreased tumor growth of NOD/SCID/IL2Rγ null mice xenograft RPMI 8226 tumor. STF-083010 was preferentially toxic to freshly isolated human CD138+ MM cells compared with other similarly isolated cell populations[2]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| SF21 cell | Function assay | Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM | 24749861 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.75mL 3.15mL 1.58mL |
31.51mL 6.30mL 3.15mL |
| 参考文献 |
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