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Formula | C22H28N4O2 |
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Molecular Weight | 380.48 | CAS No. | 1616391-87-7 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 76 mg/mL (199.74 mM) | ||||||||
Ethanol | 76 mg/mL (199.74 mM) | ||||||||||
Water | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM. | ||
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Targets |
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In vitro | In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[2][3]. |
Animal Study: |
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Data from [Data independently produced by , , Cancer Med, 2018, 7(3):869-882]
(S)-2-(Cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide Attenuates RANKL-Induced Osteoclast Differentiation by Inhibiting NF-κB Nuclear Translocation [ Int J Mol Sci, 2023, 24(5)4327] | PubMed: 36901758 |
Global profiling of arginine dimethylation in regulating protein phase separation by a steric effect-based chemical-enrichment method [ Proc Natl Acad Sci U S A, 2022, 119(43):e2205255119] | PubMed: 36256816 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
PRMT5 Inhibition Promotes PD-L1 Expression and Immuno-Resistance in Lung Cancer [ Front Immunol, 2021, 12:722188] | PubMed: 35111150 |
An AKT/PRMT5/SREBP1 axis in lung adenocarcinoma regulates de novo lipogenesis and tumor growth [ Cancer Sci, 2021, 10.1111/cas.14988] | PubMed: 34033176 |
Arginine methylation of SHANK2 by PRMT7 promotes human breast cancer metastasis through activating endosomal FAK signalling [ Elife, 2020, 9e57617] | PubMed: 32844749 |
Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition. [ J Immunother Cancer, 2019, 7(1):277] | PubMed: 31653272 |
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
PRMT 5 promotes cell proliferation by inhibiting BTG 2 expression via the ERK signaling pathway in hepatocellular carcinoma [Jiang H Cancer Med, 2018, 7(3):869-882] | PubMed: 29441724 |
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Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.