Metarrestin (ML246) 破坏核仁结构并抑制 RNA 聚合酶 (Pol) I 转录，部分是通过与翻译延伸因子 eEF1A2 相互作用。Metarrestin 是一种一流的核周区室抑制剂，具有良好的 PK 特性，可有效抑制转移。
货号:ajcx14450
CAS:1443414-10-5
分子式:C31H30N4O
分子量：474.6
溶解度:DMSO: 31.25 mg/mL (65.84 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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).