Rbin-1 Chemical Properties

Boiling point:

479.6±47.0 °C(Predicted)

Density 

1.34±0.1 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

Soluble in DMSO (up to at least 25 mg/ml)

pka

10.34±0.50(Predicted)

form 

solid

color 

Pale yellow

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Rbin-1 Usage And Synthesis

Description

Rbin-1 is a triazinoindole inhibitor of midasin (mdn1), an essential protein for eukaryotic ribosome biogenesis. It inhibits the growth of fission yeast strains in vitro (GI₅₀ = 136 nM) and inhibits mdn1 ATPase activity by approximately 40% when used at a concentration of 1 μM. Rbin-1 inhibits pre-rRNA processing and nuclear export of the pre-60S ribosome subunit in mdn1-ts, but not mdn1-F1093L mutant, S. pombe cells. It also decreases ribosome assembly protein 4 (Rsa4) levels in Rix1 particles, a ribosome assembly intermediate, Rix1-bound Ytm1 levels, and Rix7 and Ppp1 levels in the nucleolar pre-60S particle Nsa1 in mdn1-ts fission yeast cells.

Uses

3-[(2-Methyl-2-propen-1-yl)thio]-5H-1,2,4-triazino[5,6-b]indole is a triazinoindole derivative that inhibits eukaryotic ribosome biogenesis (1). It is also an ATPase inhibitor (1).

Definition

ChEBI: 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.

References

[1] SHIGEHIRO A. KAWASHIMA. Potent, Reversible, and Specific Chemical Inhibitors of Eukaryotic Ribosome Biogenesis[J]. Cell, 2016, 167 1: 512-524.e14. DOI:10.1016/j.cell.2016.08.070

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