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Product Details

GSK3326595 | Selective PRMT5 inhibitor

GSK3326595 (1616395-22-3) 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

References/Citations
1) Gerhart et al. (2018), Activation of the p53-MDM4 regulatory axis defines the anti-tumor response to PRMT5 inhibition through its role in regulating cellular splicing; Sci. Rep. 8 9711
2) AbuHammad et al. (2019), Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma; Proc. Natl. Acad. Sci. USA 116 179909
3) NCT02783300

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Catalog#  10-4028-0005

$50.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1616392-22-3
Catalog Number:
10-4028
Activity:
Selective PRMT5 inhibitor
Chemical Name:
6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide
Alternate Name:
EPZ015938
Molecular Weight:
452.56
Molecular Formula:
C24H32N6O3
Solubility:
Soluble in DMSO (up to 20 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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