Metarrestin (Synonyms: ML246) |
| Katalog-Nr.GC38201 |
Metarrestin (ML246) ist ein oral aktiver, erstklassiger und spezifischer Inhibitor des perinukleolÄren Kompartiments. Metarrestin unterbricht die nukleolÄre Struktur und hemmt die Transkription der RNA-Polymerase (Pol) I, zumindest teilweise durch Wechselwirkung mit dem Translationselongationsfaktor eEF1A2. Metarrestin blockiert die Entwicklung von Metastasen und verlÄngert das Überleben in Maus-Krebsmodellen.
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Cas No.: 1443414-10-5
Sample solution is provided at 25 µL, 10mM.
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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].
[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).
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