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10-4028

GSK3326595

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£149.00

SKU:
10-4028
Additional Names:
EPZ015938
Physical State:
Solid
Molecular Weight:
452.56
Purity:
98%
Purification:
HPLC Purified
Storage Conditions:
-20[o]C
Supplier:
Focus Biomolecules
CAS Number:
1616392-22-3
Immunogen:
Protein methyltransferase|RNA
Extra Details:
GSK3326595 is a potent (IC50 = 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5.1 PRMT5 inhibition activated the p53 pathway via induction of alternative splicing of MDM4 leading to a potent anti-proliferative response both in vitro and in vivo. Combination therapy with palbociclib (CDK4/6 inhibitor, Focus Cat.# 10-4760) and GSK3326595 lead to increased efficacy of palbociclib in treating native and resistant models of melanoma via regulation of the PRMT5-MDM4 axis.2 Currently in clinical Trials.3
Shipping Conditions:
Ambient