341329
Fatostatin hydrobromide
A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 precursors to the active nuclear forms by blocking SREBPs-SCAP ER to Golgi translocation.
别名:
Fatostatin, 125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
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关于此项目
经验公式（希尔记法）:
C18H18N2S · xHBr
化学文摘社编号:
分子量:
294.41 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
Fatostatin, A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 precursors to the active nuclear forms by blocking SREBPs-SCAP ER to Golgi translocation.
SMILES string
[s]1c(nc(c1)c3ccc(cc3)C)c2cc(ncc2)CCC.Br
InChI
1S/C18H18N2S.BrH/c1-3-4-16-11-15(9-10-19-16)18-20-17(12-21-18)14-7-5-13(2)6-8-14;/h5-12H,3-4H2,1-2H3;1H
InChI key
RJCFNQZVFUMORB-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
pale yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 µM in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functions in vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 µg/ml) and IGF1-dependent DU-145 proliferation (IC50 = 100 nM), and exhibits in vivo efficacy in lowering blood glucose level (by 70%) and body weight (by 12%) of ob/ob mice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.
Other Notes
Kamisuki, S., et al. 2009. Chem. Biol.16, 882.
Choi, Y., et al. 2003. J. Biol. Chem.278, 7320.
Choi, Y., et al. 2003. J. Biol. Chem.278, 7320.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Athina Maniscalchi et al.
Redox biology, 71, 103074-103074 (2024-02-18)
Brain iron accumulation constitutes a pathognomonic indicator in several neurodegenerative disorders. Metal accumulation associated with dopaminergic neuronal death has been documented in Parkinson's disease. Through the use of in vivo and in vitro models, we demonstrated that lipid dysregulation manifests
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