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Metarrestin

Chemical Structure : Metarrestin

CAS No.: 1443414-10-5

Metarrestin (ML246;ML 246)

Catalog No.: PC-35083Not For Human Use, Lab Use Only.

Metarrestin (ML246) is a specific inhibitor of perinuclear compartment (PNC), disrupts PNCs in PC3M-GFP-PTB cells with IC50 of 0.39 uM, specifically binds eEF1A2.

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Biological Activity

Metarrestin (ML246) is a specific inhibitor of perinuclear compartment (PNC), disrupts PNCs in PC3M-GFP-PTB cells with IC50 of 0.39 uM, specifically binds eEF1A2.
Metarrestin (ML246) reduces PNC prevalence in different human cancer cell lines at 1 uM (IC100 for PC3M cells) for 24 hours.
Metarrestin (ML246) disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, by interacting with the translation elongation factor eEF1A2inhibits cancer cell invasion in vitro, suppresses metastatic development in three mouse models of human cancer, and extends survival of mice in a metastatic pancreatic cancer xenograft model with no organ toxicity or discernable adverse effects.

Physicochemical Properties

M.Wt 474.608
Formula C31H30N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Trans-4-(7-benzyl-4-imino-5,6-diphenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-3-yl) cyclohexanol

References

1. Frankowski KJ, et al. Sci Transl Med. 2018 May 16;10(441). pii: eaap8307.

2. Frankowski K, et al. Discovery and Development of Small Molecules That Reduce PNC Prevalence.Probe Reports from the NIH Molecular Libraries Program [Internet].

3. Rocchi A, et al. PLoS Genet. 2017 Aug 14;13(8):e1006962.

4. Kuramoto K, et al. Autophagy. 2016 Sep;12(9):1460-71.

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