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 (GI
50 = 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) Kawashime?et al.?(2016),?Potent, Reversible, and Specific Chemical Inhibitors of Eukaryotic Ribosome Biogenesis; Cell?167?512
