Description
ChemicalBook > CAS DataBase List > GSK591

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

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8418
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55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
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60
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4566
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
1005
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55
D&C Chemicals
Tel
+86-21-58447131
Fax
+86-21-61642470
Email
1724405207@qq.com
Country
China
ProdList
472
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55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2990
Advantage
58

1616391-87-7, GSK591Related Search:


  • 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