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.
別名:
Fatostatin, 125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
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この商品について
実験式（ヒル表記法）:
C18H18N2S · xHBr
CAS番号:
分子量:
294.41 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
製品名
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.
Quality Segment
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
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
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.
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。