GSK3326595(EPZ015938) , 99% , 1616392-22-3
| Pack Size | Price | Stock | Quantity |
| 5mg | RMB551.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| 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). |
| pka | 12.44±0.46(Predicted) |
| form | solid |
| 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. |
| InChIKey | JLCCNYVTIWRPIZ-NRFANRHFSA-N |
| SMILES | C1=NC(NC2CCN(C(C)=O)CC2)=CC(C(NC[C@H](O)CN2CCC3=C(C2)C=CC=C3)=O)=N1 |
Description and Uses
GSK3326595 (1616395-22-3) is a potent (IC50= 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5.1PRMT5 inhibition activated the p53 pathwayviainduction of alternative splicing of MDM4 leading to a potent anti-proliferative response bothin vitroandin 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.2Currently in clinical trials.3
GSK-3326595 is a protein arginine methyltransferase 5(PRMT5) inhibitor under clinical trial.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 |
