GSK837149A

Modify Date: 2025-09-22 09:03:46

GSK837149A Structure
GSK837149A structure
Common Name GSK837149A
CAS Number 13616-29-0 Molecular Weight 554.60100
Density N/A Boiling Point N/A
Molecular Formula C23H22N8O5S2 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of GSK837149A


GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer[1][2].

 Names

Name N,N'-bis-(4-methyl-pyrimidin-2-yl)-4,4'-carbonyldiamino-bis-benzenesulfonamide
Synonym More Synonyms

 GSK837149A Biological Activity

Description GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer[1][2].
Related Catalog
Target

Ki: 30 nM (type I FASN)[1]

In Vitro GSK837149A (0.1 nM-0.1 mM) 对乙酰辅酶 A/丙二酰辅酶 A 和乙酰乙酰辅酶 A 的抑制作用随作用浓度增加而增强[1]。
References

[1]. Vázquez MJ, et al. Discovery of GSK837149A, an inhibitor of human fatty acid synthase targeting the beta-ketoacyl reductase reaction. FEBS J. 2008 Apr;275(7):1556-1567.  

[2]. Singha PK, et al. Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells. Eur J Pharm Sci. 2020 Apr 7;149:105321.  

 Chemical & Physical Properties

Molecular Formula C23H22N8O5S2
Molecular Weight 554.60100
Exact Mass 554.11500
PSA 201.79000
LogP 5.58260
InChIKey RSINKZJTTORDAJ-UHFFFAOYSA-N
SMILES Cc1ccnc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(S(=O)(=O)Nc4nccc(C)n4)cc3)cc2)n1
Storage condition 2-8°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H319
Precautionary Statements P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi
RIDADR NONH for all modes of transport

 GSK837149ABioassay

View more

Name: Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
Source: NCGC
Target: N/A
External Id: SERCaMPGLuc-p1-antagonist
Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
Name: Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ...
Source: NCGC
External Id: huntington-HTTAS8-p1-FF-overN
Name: Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
Source: NCGC
Target: N/A
External Id: TRND-SARS-CoV-2-cytotox-48hr
Name: Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
Source: NCGC
External Id: TRND-SARS-CoV-2-PP
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OPM1-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-OC1MY5-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-KMS_34-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_L363-m4-1
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 Synonyms

N,N'-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea
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