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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
RBIN-1
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
328023-11-6
- 规格:
100mg/50mg/25mg/10mg/5mg
| 规格: | 100mg | 产品价格: | ¥5838.0 |
|---|---|---|---|
| 规格: | 50mg | 产品价格: | ¥4354.0 |
| 规格: | 25mg | 产品价格: | ¥2790.0 |
| 规格: | 10mg | 产品价格: | ¥1290.0 |
| 规格: | 5mg | 产品价格: | ¥790.0 |
| 基本信息 | |
| CAS | No.328023-11-6 |
| 英文名称 | RBIN-1 |
| 别名 | Ribozinoindole-1;Rbin-1 |
| 分子式 | C13H12N4S |
| 分子量 | 256.33 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD02369534 |
| SMILES | C=C(C)CSC1=NN=C2C(NC3=C2C=CC=C3)=N1 |
| 靶点 | Mdn1 |
| 通路 | DNA Damage/DNA Repair |
| 背景说明 | Rbin-1是有效的真核核糖体组装的化学抑制剂。 |
| 生物活性 | Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).[1] |
| IC50 | GI50=136±7 nM (ATPase)[1] |
| In Vitro | Rbin-1 is a potent and reversible triazinoindole-based inhibitors of eukaryotic ribosome biogenesis. Rbin-1 inhibits recombinant full-length Mdn1s ATPase activity. Two of the active analogs (Rbin-1 and Rbin-2) inhibit the ATPase activity by 40% at 1 uM. In particular, an analog (Rbin-2) with a bromine substituent at postion-7 is 10-fold more active than Rbin-1 (GI50=14±1 nM (Rbin-2); 136±7 nM (Rbin-1), n=4, mean±SD)[1]. |
| 激酶实验 | Radioactive γ-P32-ATP is added to 600 mM MgATP (pH=7) solutions at volume ratios of 1:1000-1:300, depending on the lifetime of the radioactive reagent. The total volume of each reaction is 12 mL, including 6 ml of protein from size exclusion chromatography fractions (final concentration 0-50 nM for different fractions, peak fractions are used for Rbin-1 and AMPPNP inhibition), 4 mL FPLC SEC buffer with 0.6 mM Na2SO4 and 2 mL MgATP (final concentration=100 mM). The reactions are then incubated at room temperature for 30 or 60 min before quenching with 12 mL 0.2 M EDTA. 1 mL from each reaction mixture is spotted on to TLC PEI cellulose F plates. The TLC buffer contained 0.15 M formic acid and 0.15 M lithium chloride. The TLC plates are then imaged using the Typhoon Scanner 9400. ImageJ is used to calculate the densitometric ratio of the spots corresponding to radioactive free phosphate and ATP to determine the percent of ATP hydrolyzed[1]. |
| 数据来源文献 | [1]. Kawashima SA, et al. Potent, Reversible, and Specific Chemical Inhibitors of Eukaryotic Ribosome Biogenesis. Cell. 2016 Oct 6;167(2):512-524.e14. |
| 单位 | 瓶 |
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