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13616-29-0

13616-29-0 structure
13616-29-0 structure
  • Name: GSK837149A
  • Chemical Name: N,N'-bis-(4-methyl-pyrimidin-2-yl)-4,4'-carbonyldiamino-bis-benzenesulfonamide
  • CAS Number: 13616-29-0
  • Molecular Formula: C23H22N8O5S2
  • Molecular Weight: 554.60100
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Fatty Acid Synthase (FAS)
  • Create Date: 2017-12-21 01:13:35
  • Modify Date: 2024-01-11 00:28:08
  • 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].

Name N,N'-bis-(4-methyl-pyrimidin-2-yl)-4,4'-carbonyldiamino-bis-benzenesulfonamide
Synonyms N,N'-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea
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.  

Molecular Formula C23H22N8O5S2
Molecular Weight 554.60100
Exact Mass 554.11500
PSA 201.79000
LogP 5.58260
Storage condition 2-8°C
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
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