EPZ-015866( GSK-591 | GSK-3203591 )

Catalog No. M12360 CAS No. 1616391-87-7

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HNMR

HPLC

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Product Name

EPZ-015866
Note

Research use only, not for human use.
Brief Description

EPZ-015866 (GSK-591, GSK-3203591) is a potent, selective protein methyltransferase 5 (PRMT5) inhibitor with IC50 of 4 nM.
Description

EPZ-015866 (GSK-591, GSK-3203591) is a potent, selective protein methyltransferase 5 (PRMT5) inhibitor with IC50 of 4 nM; shows excellent selectivity against other PMT enzymes observed with EPZ015666; inhibits the proliferation of Z-138 cells with IC50 of 62 nM.
In Vitro

GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro. Cell Proliferation Assay Cell Line:MCF7, T47D, and MCF10A cells Concentration:5 μM Incubation Time:Result:Suppressed BCSCs proliferation and self-renewal.
In Vivo

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Synonyms

GSK-591 | GSK-3203591
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

PRMT5
Research Area

Other Indications
Indication

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CAS Number

1616391-87-7
Formula Weight

380.4833
Molecular Formula

C22H28N4O2
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4CCC4)=NC=C3
Chemical Name

4-Pyridinecarboxamide, 2-(cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-

1. Duncan KW, et al. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. 2.?Gerhart SV, et al. Sci Rep. 2018 Jun 26;8(1):9711.

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