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Pemrametostat (GSK3326595)

Names

[ CAS No. ]:
1616392-22-3

[ Name ]:
Pemrametostat (GSK3326595)

[Synonym ]:
6-[(1-Acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-4-pyrimidinecarboxamide
4-Pyrimidinecarboxamide, 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-
EPZ-015938

Biological Activity

[Description]:

GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Research Areas >> Cancer

[Target]

IC50: 6.2 nM (PRMT5)[1]


[In Vitro]

GSK3326595 (EPZ015938), has entered clinical trials for the treatment of solid tumors and non-Hodgkin’s lymphoma[1].

[References]

[1]. WO 2016022605 A1


[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591) | Chaetocin

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
760.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H32N6O3

[ Molecular Weight ]:
452.549

[ Flash Point ]:
413.6±32.9 °C

[ Exact Mass ]:
452.253601

[ LogP ]:
2.88

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.626

[ Storage condition ]:
-20℃

Related Compounds