GSK-3326595

CAS NO.：1616392-22-3
Empirical Formula: C24H32N6O3
Molecular Weight: 452.55
MDL number: MFCD29991177
Update Date: 2024-11-19 23:02:33

What is GSK-3326595?

Description

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

The Uses of GSK-3326595

GSK-3326595 is a protein arginine methyltransferase 5(PRMT5) inhibitor under clinical trial.

References

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

Properties of GSK-3326595

Boiling point:	760.3±60.0 °C(Predicted)
Density	1.275±0.06 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
solubility	Soluble in DMSO (up to 20 mg/ml).
form	solid
pka	12.44±0.46(Predicted)
color	Off-white
Stability:	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.