GSK-3326595
- CAS NO.：1616392-22-3
- Empirical Formula: C24H32N6O3
- Molecular Weight: 452.55
- MDL number: MFCD29991177
- Update Date: 2026-03-13 23:13:44
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. |
Safety information for GSK-3326595
Computed Descriptors for GSK-3326595
New Products
Mirtazapine Impurity C/Mirtazapine Lactam Impurity Cyclopropane-1,1-dicarboxylic acid [1]Benzothieno[2,3-c]pyridine, 1,7-dichloro-8-methyl- (S)-3-Fluoro-pyrrolidine hydrochloride Cyclobutylamine 1-Bromo-2-Methoxy-3-Nitrobenzene 3-Oxocyclobutane-1-carboxylicacid (4-Bromophenyl)(3,4-dimethoxyphenyl)methanone N-Nitroso hydroxy Cetrizine EP Impurity-A Noradrenaline EP Impurity D/Noradrenaline Methyl Ether Cetirizine EP Impurity A/Cetirizine CBHP Impurity Lantanoprost rc B Clidinium Bromide Impurity 2-chloro-7-cyclopentyl-N,N-dimethylpyrrolo [2,3-d]pyrimidine-6-carbox amide 4-amino-2-fluoro-N- methylbenzamide N-(2-chloropyrimidin-4-yl)-N,2,3- trimethyl-2H- indazol 6-amine 5-Chloro-3- Methyl -1,3-2-benzoxazol-2(3H)-one 4-Bromo-2-fluoro-N-methylbenzamide N-Boc-1,4-butanediamine 4-Dimethylamino pyridine 2-Chlorotrityl Chloride 4-Bromoaniline 5-Bromo-2-chlorobenzoic acid 1,2,3,9-Tetrahydro-4(H)-carbazol-4-oneRelated products of tetrahydrofuran
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