| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
Rbin-1 (also known as ribozinoindole-1) is a potent and specific chemical inhibitor of eukaryotic ribosome assembly. It blocks the ATPase activity of recombinant full-length Mdn1 in vitro. In order to investigate the mechanism of action of Rbin-1, resistant clones that were able to proliferate in the presence of Rbin-1 were isolated from MDR-sup fission yeast cells through chemical mutagenization. The mdn1 gene contained one of five distinct point mutations, according to the results, in each of the 13 Rbin-1 resistant clones.
| Targets |
ATPase ( GI50 = 136±7 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Depending on the radioactive reagent's lifetime, volume ratios of 1:1000–1:300 are used when adding radioactive γ-P32-ATP to 600 mM MgATP (pH=7) solutions. The total volume of each reaction is 12 mL, which includes 4 mL of FPLC SEC buffer with 0.6 mM Na2SO4 and 2 mL of MgATP (final concentration=100 mM), 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). Following a 30- to 60-minute incubation period at room temperature, the reactions are quenched with 12 mL of 0.2 M EDTA. On TLC PEI cellulose F plates, 1 mL of each reaction mixture is spotted. Formic acid (0.15 M) and lithium chloride (0.15 M) were present in the TLC buffer. Following that, the Typhoon Scanner 9400 is used to image the TLC plates. Utilizing ImageJ, compute the densitometric ratio between the spots that represent radioactive free phosphate and ATP to ascertain the percentage of ATP that has been hydrolyzed[1].
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| Cell Assay |
Enzymatic ribosome assembly is strongly inhibited by ribozinoindoles. Mdn1 or the cellular processes that use this protein are the target of Rbin-1. It successfully prevents yeast cells from growing.
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| Animal Protocol |
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| References | |||
| Additional Infomation |
Ribozinoindole-1 is a triazinoindole that is 5H-[1,2,4]triazino[5,6-b]indole which is substituted at position 3 by a (2-methylprop-2-en-1-yl)thio group. A potent inhibitor of midasin which is an essential protein for eukaryotic ribosome biogenesis. It is a triazinoindole and an organic sulfide.
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| Molecular Formula |
C13H12N4S
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| Molecular Weight |
256.33
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| Exact Mass |
256.078
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| Elemental Analysis |
C, 60.92; H, 4.72; N, 21.86; S, 12.51
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| CAS # |
328023-11-6
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| Related CAS # |
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| PubChem CID |
5731061
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
479.6±47.0 °C at 760 mmHg
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| Flash Point |
243.8±29.3 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.718
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| LogP |
3.28
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
322
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])C(=C([H])[H])C([H])([H])[H])C1N=NC2=C(N=1)N([H])C1=C([H])C([H])=C([H])C([H])=C12
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| InChi Key |
LPCWHNSRTRBKBO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12N4S/c1-8(2)7-18-13-15-12-11(16-17-13)9-5-3-4-6-10(9)14-12/h3-6H,1,7H2,2H3,(H,14,15,17)
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| Chemical Name |
3-(2-methylprop-2-enylsulfanyl)-5H-[1,2,4]triazino[5,6-b]indole
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (6.52 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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