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Rbin-1 (Synonyms: Ribozinoindole-1)

Cat. No.: HY-100816 Purity: 99.91%
Handling Instructions

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).

For research use only. We do not sell to patients.

Rbin-1 Chemical Structure

Rbin-1 Chemical Structure

CAS No. : 328023-11-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 310 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1000 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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).

IC50 & Target

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 Mdn1’s 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].

Molecular Weight

256.33

Formula

C₁₃H₁₂N₄S

CAS No.

328023-11-6

SMILES

C=C(C)CSC1=NN=C2C(NC3=C2C=CC=C3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (120.94 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.67 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.67 mg/mL (6.52 mM); Precipitated solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Rbin-1Ribozinoindole-1Rbin1Rbin 1Ribozinoindole1Ribozinoindole 1OthersInhibitorinhibitorinhibit

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Rbin-1
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HY-100816
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