Metarrestin (Synonyms: ML246) |
| カタログ番号GC38201 |
メタレスチン (ML246) は、経口で活性なファーストインクラスの特定の核周囲コンパートメント阻害剤です。メタレスチンは、翻訳伸長因子 eEF1A2 と相互作用することにより、核小体構造を破壊し、RNA ポリメラーゼ (Pol) I 転写を少なくとも部分的に阻害します。メタレスチンは、マウス癌モデルの転移発生をブロックし、生存期間を延長します。
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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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