A PRMT5 inhibitor
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GSK3326595

Item No. 27305

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-4-pyrimidinecarboxamide
CAS Number
1616392-22-3
Molecular Formula
C24H32N6O3
Formula Weight
452.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
249 nm
SMILES
O=C(C1=CC(NC2CCN(C(C)=O)CC2)=NC=N1)NC[C@H](O)CN3CC4=CC=CC=C4CC3
InChi Code
InChI=1S/C24H32N6O3/c1-17(31)30-10-7-20(8-11-30)28-23-12-22(26-16-27-23)24(33)25-13-21(32)15-29-9-6-18-4-2-3-5-19(18)14-29/h2-5,12,16,20-21,32H,6-11,13-15H2,1H3,(H,25,33)(H,26,27,28)/t21-/m0/s1
InChi Key
JLCCNYVTIWRPIZ-NRFANRHFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).1 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.

    WARNING This product is not for human or veterinary use.