Rbin-1
(Synonyms: Ribozinoindole-1) 目录号 : GC15407
An inhibitor of midasin
Cas No.:328023-11-6
Sample solution is provided at 25 µL, 10mM.
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Rbin-1 is an eukaryotic ribosome assembly inhibitor.
All cellular proteins are synthesized by ribosomes, whose biogenesis is a complex multi-step process quickly completed in eukaryotes. Several chemical inhibitors of ribosome function are available, however, potent validated chemical probes are still lacking to analyze the dynamics of eukaryotic ribosome assembly.
In vitro: In the mode of action study of Rbin-1, the MDR-sup fission yeast cells was chemically mutagenized and the resistant clones that can grow in the presence of Rbin-1 were isolated. Results found that each of the 13 Rbin-1 resistant clones had one of five different point mutations in the mdn1 gene. It was further confirmed that, using overexpression on plasmids in MDR-sup cells and by replacement of endogenous mdn1 in wild-type cells, all the identified mutations were enough to confer resistance to Rbin-1. In addition, Rbin-1 at 1 μM was able to inhibit the ATPase activity by around 40%. Moreover, the nuclear export of the pre-40S subunits that were tracked using two different reporters, Rps3- GFP and Rps2-GFP, could not be blocked in Rbin-1-treated cells, suggesting that Mdn1 had specific roles in pre-60S ribosome assembly [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, Rbin-1 is still in the preclinical development stage.
Reference:
[1] Kawashima SA, Chen Z, Aoi Y, Patgiri A, Kobayashi Y, Nurse P, Kapoor TM. Potent, Reversible, and Specific Chemical Inhibitors of Eukaryotic Ribosome Biogenesis. Cell. 2016 Oct 6;167(2):512-524.e14.
Kinase experiment: | 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]. |
References: [1]. Kawashima SA, et al. Potent, Reversible, and Specific Chemical Inhibitors of Eukaryotic Ribosome Biogenesis. Cell. 2016 Oct 6;167(2):512-524.e14. | |
| Cas No. | 328023-11-6 | SDF | |
| 别名 | Ribozinoindole-1 | ||
| 化学名 | 3-((2-methylallyl)thio)-5H-[1,2,4]triazino[5,6-b]indole | ||
| Canonical SMILES | C=C(C)CSC1=NC2=C(N=N1)C3=CC=CC=C3N2 | ||
| 分子式 | C13H12N4S | 分子量 | 256.33 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9012 mL | 19.5061 mL | 39.0122 mL |
| 5 mM | 0.7802 mL | 3.9012 mL | 7.8024 mL |
| 10 mM | 0.3901 mL | 1.9506 mL | 3.9012 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet