Metarrestin

Names

[ Name ]:
Metarrestin

Biological Activity

[Description]:

Metarrestin (ML246) disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

[Target]

RNA polymerase (Pol) I[1][2]

[References]

[1]. Vilimas T, et al. Pharmacokinetic evaluation of the PNC disassembler metarrestin in wild-type and Pdx1-Cre;LSL-KrasG12D/+;Tp53R172H/+ (KPC) mice, a genetically engineered model of pancreatic cancer. Cancer Chemother Pharmacol. 2018 Dec;82(6):1067-1080.

[2]. Frankowski KJ, et al. Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis. Sci Transl Med. 2018 May 16;10(441).

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₁H₃₀N₄O

[ Molecular Weight ]:
474.60

[ Storage condition ]:
-20°C

Related Compounds

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