GSK-3326595 manufacturers
- GSK3326595
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- $39.00
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2026-07-27
- CAS:1616392-22-3
- Purity: 98.88%
- Supply Ability: 10g
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| | GSK-3326595 Basic information |
| Product Name: | GSK-3326595 | | Synonyms: | 6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamide;4-Pyrimidinecarboxamide, 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-;GSK-3326595,EPZ-015938;EPZ-015938 (GSK3326595);4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamid;6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1;EPZ015938; 6-[(1-ACETYLPIPERIDIN-4-YL)AMINO]-N-[(2S)-2-HYDROXY-3-(1;2;3;4-TETRAHYDROISOQUINOLIN-2-YL)PROPYL]PYRIMIDINE-4-CARBOXAMID;EPZ015938; EPZ 015938; EPZ-015938 | | CAS: | 1616392-22-3 | | MF: | C24H32N6O3 | | MW: | 452.55 | | EINECS: | | | Product Categories: | API | | Mol File: | 1616392-22-3.mol |  |
| | GSK-3326595 Chemical 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 |
| | GSK-3326595 Usage And Synthesis |
| Description | GSK3326595 (1616395-22-3) is a potent (IC50= 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5.1PRMT5 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 | | Uses | GSK-3326595 is a protein arginine methyltransferase 5(PRMT5) inhibitor under clinical trial. | | in vivo | GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9weeks) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice[3].
GSK3326595 (25-50 mg/kg, Oral, once a day for 2weeks) enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice[5]. | Animal Model: | LDL receptor knockout mice[3] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Did not alter atherosclerosis susceptibility.
Increased hepatic triglyceride levels without changing the hyperlipidemia extent.
Activated genes involved in fatty acid acquisition. |
| Animal Model: | myelocytomatosis transgene turned on mice[5] | | Dosage: | 25 mg/kg, 50 mg/kg | | Administration: | Oral | | Result: | Significantly suppressed tumor growth at 50 mg/kg.
Showed better therapeutic efficacy at 25 mg/kg. |
| | IC 50 | PRMT5; CDK4; CDK6 | | References | [1] SARAH V GERHART. Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.[J]. Scientific Reports, 2018: 9711. DOI:10.1038/s41598-018-28002-y
[2] SHATHA ABUHAMMAD. Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2019, 116 1: 17990-18000. DOI:10.1073/pnas.1901323116 |
| | GSK-3326595 Preparation Products And Raw materials |
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