In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 7.7 nM
GSK 2194069 is a potent human fatty acid synthase inhibitor.
Human fatty acid synthase (hFAS) is a multifunctional enzyme solely responsible for the de novo synthesis of long chain fatty acids. hFAS is expressed highly in a number of cancers, while with low observed expression in most normal tissues. Though normal tissues get fatty acids from the diet, tumor tissues can rely on de novo fatty acid synthesis, which makes hFAS an attractive metabolic target for cancer treatment.
In vitro: GSK2194069 displayed acceptable solubility and permeability and thus was chosen for further characterization. GSK2194069 had an IC50 of 29 ± 3.2 nM versus hFAS with acetoacetyl-CoA as the substrate but showed little or no inhibition with crotonyl-CoA andβ-hydroxybutyryl-CoA. GSK2194069 was also found not to inhibit the partial activities of the KS domain .
In vivo: In those mice dosed with GSK2194069, tumour growth was inhibited. There was no significant weight loss in the GSK2194069 treated group and no adverse effects were observed. The effect of GSK2194069 in decreasing acetate uptake was demonstrated by scintillation detection of C42b xenograft tumours by 56% 2 hours after dosing with GSK2194069. Inhibition of FAS caused by GSK2194069 led to a decrease in acetate signal in all animals .
Clinical trial: N/A
 Hardwicke MA,Rendina AR,Williams SP,Moore ML,Wang L,Krueger JA,Plant RN,Totoritis RD,Zhang G,Briand J,Burkhart WA,Brown KK, Parrish CA. A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol.2014 Sep;10(9):774-9.
 Greg Shaw, David Lewis, Joan Boren, Antonio Ramos-Montoya, Robert Bielik, Dmitry Soloviev, Brindle Kevin, Neal David. 509 THERAPEUTIC FATTY ACID SYNTHASE INHIBITION IN PROSTATE CANCER AND THE USE OF 11C-ACETATE TO MONITOR THERAPEUTIC EFFECTS. The Journal of Urology. 2013Volume 189, Issue 4, Supplement, Pagese208–e209
|Physical Appearance||White solid|
|Storage||Desiccate at -20°C|
|Solubility||Soluble in DMSO|
|Canonical SMILES||O=C1NN=C(C[[email protected]@H]2CCN(C(C3CC3)=O)C2)N1C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|