GSK591

Description

Product Name: GSK591
CAS No.: 1616391-87-7
Chemical Name: GSK591
Synonyms: GSK591;GSK592;CS-2179;EPZ015866;GSK3203591;GSK-3203591;GSK 3203591;EPZ015866(GSK591);GSK-591(EPZ-15866);GSK591 (EPZ-015866)
CBNumber: CB33122823
Molecular Formula: C22H28N4O2
Formula Weight: 380.48
MOL File: 1616391-87-7.mol

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GSK591 Property

Boiling point:: 648.4±55.0 °C(Predicted)
Density: 1.252±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: ≥38 mg/mL in DMSO; insoluble in H2O; ≥15.4 mg/mL in EtOH
form: powder
pka: 13.54±0.46(Predicted)
color: white to beige

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1751
Product name: GSK591
Purity: ≥97% (HPLC)
Packaging: 5MG
Price: $107
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1751
Product name: GSK591
Purity: ≥97% (HPLC)
Packaging: 25MG
Price: $434
Updated: 2023/06/20

Cayman Chemical

Product number: 18354
Product name: GSK591
Purity: ≥95%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 18354
Product name: GSK591
Purity: ≥95%
Packaging: 5mg
Price: $93
Updated: 2024/03/01

Cayman Chemical

Product number: 18354
Product name: GSK591
Purity: ≥95%
Packaging: 10mg
Price: $169
Updated: 2024/03/01

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GSK591 Chemical Properties,Usage,Production

Description

GSK591 is a chemical probe of PRMT5 (protein arginine methyltransferase 5), which plays a key role in various biological processes. PRMT5 is related to many human diseases including certain cancers like mantle cell lymphoma (MCL). Therefore, GSK591 is a useful tool for testing biological and therapeutic hypotheses. Study has shown that it can potential inhibit the PRMT5/MEP50 complex and symmetric arginine methylation of SMD3.

Biological Activity

gsk591 is a prmt5 inhibitor.protein arginine methyltransferase-5 (prmt5) is found to have a critical role in various cellular processes such as tumorigenesis, and the overexpression of prmt5 is observed in cell lines and primary patient samples derived from lymphomas, especially mantle cell lymphoma.

Biochem/physiol Actions

GSK591 is also known as 2-(cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-4-pyridinecarboxamide, EPZ015866 and GSK3203591. It prevents the systemic arginine methylation of SmD3 (small nuclear ribonucleoprotein).

in vitro

by further optimization of epz015666, an extremely potent in vitro tool analog of epz015666, gsk591, was identified. gsk591 was found to maintain excellent selectivity against other pmt enzymes, which was similar to that of epz015666. in addition, gsk591 was shown to be an extremely potent compound suitable for in vitro studies with excellent hlm stability [1].

in vivo

in mouse pk studies, gsk591, epz015666 and their analogs showed moderate to high plasma clearance and a wide range of oral bioavailability. the volume of distribution values in these studies were from 0.6 to 45 l/kg. further pk studies demonstrated that at 100 mg/kg in mouse, the unbound plasma concentration was equivalent to or above the ic90 for a period of 12 h, therefore, indicating that the bid dosing regimen of epz015666 was able to effectively inhibit prmt5 in vivo [1].

IC 50

4 nm

References

[1] duncan kw et al. structure and property guided design in the identification of prmt5 tool compound epz015666. acs med chem lett. 2015 dec 2;7(2):162-6.

GSK591 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK591 Suppliers

China 66 United Kingdom 1 United States 9 Global 76

Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
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InvivoChem

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Fax: 708-557-7486
Email: sales@invivochem.cn
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Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
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BOC Sciences

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Aladdin Scientific

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TargetMol Chemicals Inc.

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BOC Sciences

Tel: 16314854226
Email: info@bocsci.com
Country: United States
ProdList: 9926
Advantage: 65

1616391-87-7, GSK591Related Search:

GSK8612 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol 1-(1-(3-methoxyphenyl)-7-propoxyindolizin-3-yl)ethanone GSK8612 GSK6853 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid GSK620 GSK5959 ROR gamma-t-IN-1 GSK872 3-chloro-2-(1,1-difluorobut-3-enyl)-6-methoxyquinoxaline 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)-

GSK591 (EPZ-015866)

EPZ015866

GSK591(EPZ015866,GSK3203591)

EPZ015866(GSK591)

EPZ015866,GSK3203591

GSK591

GSK3203591(EPZ015866)

EPZ-015866;EPZ 015866;GSK-591;GSK 591;GSK3203591;GSK-3203591;GSK 3203591

GSK 3203591

GSK3203591

GSK-3203591

2-(Cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydropropyl]-4-pyridinecarboxamide dihydrochloride

2-(cyclobutylamino)-N-[(2S)-2-hydroxy-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propyl]pyridine-4-carboxamide

EPZ-015866;EPZ 015866

CS-2179

(S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide

4-Pyridinecarboxamide, 2-(cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-

GSK591 >=97% (HPLC)

GSK592

GSK-591(EPZ-15866)

GSK 591,EPZ-015866,GSK591,Inhibitor,GSK 3203591,EPZ 015866,inhibit,GSK-3203591,GSK-591,Histone Methyltransferase

1616391-87-7