A PRMT5 inhibitor; inhibits methylation of peptides derived from histones H4 and H2A

GSK3326595 – 5 mg

Brand:
Cayman
CAS:
1616392-22-3
Storage:
-20
UN-No:
Non-Hazardous - /

GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).{47250} It inhibits methylation of peptides derived from the PRMT5 substrates histone H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex with IC50 values ranging from 5.9 to 19.7 nM and is more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases. GSK3326595 (200 nM) induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells and increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner. GSK3326595 inhibits growth and symmetric dimethyl arginine (SDMA) methylation in several lymphoma and breast cancer cell lines. It also reduces tumor growth in a Z-138 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg twice per day.  

 

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Description

A PRMT5 inhibitor; inhibits methylation of peptides derived from histones H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex (IC50s = 5.9-19.7 nM); more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases; induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells at 200 nM; increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner; inhibits growth and SDMA methylation in several lymphoma and breast cancer cell lines; reduces tumor growth in a Z-138 mouse xenograft model at 25, 50, and 100 mg/kg twice per day

Formal name: 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-4-pyrimidinecarboxamide

Synonyms: 

Molecular weight: 452.6

CAS: 1616392-22-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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