Fatostatin,25MG,341329-25MGCN,Sigma

销售价: ¥ 2000.54 / 件
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订货号 0BV9025
品牌型号 Sigma 341329-25MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

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.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
Quality Level100
assay≥95% (HPLC)
formsolid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,desiccated (hygroscopic),protect from light
colorpale yellow
solubilityDMSO: 10 mg/mL
shipped inambient
storage temp.2-8°C
SMILES string[s]1c(nc(c1)c3ccc(cc3)C)c2cc(ncc2)CCC.Br
InChI1S/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 keyRJCFNQZVFUMORB-UHFFFAOYSA-N
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