Fatostatin A is a cell permeable inhibitor of SREBP activation, it inhibits cancer cell proliferation by affecting mitotic microtubule spindle assembly and cell division.
|Cell lines||CHO-K1 cells|
|Preparation method||CHO-K1 cells are plated out onto a 96-well plate in medium A. The cells are transiently cotransfected with pCMV-PLAP-BP2, pCMV-SCAP, and pAc-b-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of b-galactosidase activities.|
|Incubation time||20 h|
|Animal models||Four-to-five-week-old homozygous male obese (ob/ob) mice|
|Formulation||10% DMSO in PBS|
|Dosages||30 mg/kg; 150 uL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 30 mg/mL|
Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner
Wei Shao, et al. J Lipid Res. 2016 Aug;57(8):1564-73. PMID: 27324795.
Fatostatin displays high antitumor activity in prostate cancer by blocking SREBP-regulated metabolic pathways and androgen receptor signaling
Xiangyan Li, et al. Mol Cancer Ther. 2014 Apr;13(4):855-66. PMID: 24493696.
A small molecule that blocks fat synthesis by inhibiting the activation of SREBP
Shinji Kamisuki, et al. Chem Biol. 2009 Aug 28;16(8):882-92. PMID: 19716478.
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