Fatostatin (125B11) HBr

Catalog No.S8284 Synonyms: Fatostatin A

For research use only.

Fatostatin HBr (Fatostatin A, 125B11) is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

Fatostatin (125B11) HBr Chemical Structure

CAS No. 298197-04-3

Selleck's Fatostatin (125B11) HBr has been cited by 8 Publications

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Biological Activity

Description Fatostatin HBr (Fatostatin A, 125B11) is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
Targets
SREBPs [1]
In vitro

Fatostatin inhibits the insulin-induced adipogenesis of 3T3-L1 cells and the serum-independent growth of human androgen-independent prostate cancer (DU145) cells. Fatostatin blocks the activation of SREBPs in cells in tissue culture[1]. Fatostatin suppresses cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. Fatostatin also reduced in vitro invasion and migration in both cell lines. Further, fatostatin causes G2/M cell cycle arrest and induces apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO-K1 cells M2j4SWZ2dmO2aX;uJIF{e2G7 NGLuZ2IzOCCq NFjRb2xKdmirYnn0bY9vKG:oIGPSSWJROiCjY4TpeoF1cW:wIHX4dJJme3OnZDDpckBEUE9vS{GgZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDwV3JGNUy3YzDwcIF{dWmmIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEKwJIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9OU43KM7:TR?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV4MUG1Nkc,OjF3NkGxOVI9N2F-
mouse hepatocytes M3OzdWZ2dmO2aX;uJIF{e2G7 M1fKU|EhfU1? NHvpOGY6OCCvaX7z NELHbnhO\XSjYn;sbYMhe3SjYnnsbZR6KGmwIH3veZNmKGincHH0c4N6fGW|IHH0JFEhfU1iYX\0[ZIhQTBibXnud{BjgSCOQz3NV{9OWyCjbnHsfZNqew>? MoK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3NkGxOVIoRjJzNU[xNVUzRC:jPh?=
InhA cells M1fmO2FvfGmvaXPyc4Jq[WxiYYPzZZk> Ml:2RY51cW2rY4LvZolidCCjY4Tpeol1gSCjZ3HpcpN1KE27Y3;iZYN1\XKrdX2geJVj\XKldXzvd4l{KEh|N2L2JI93\XJvZYjwdoV{e2mwZzDJcohCKGOnbHzzJIF{e2W|c3XkJIF{KHWyc3jp[pQhd2ZiTVnDJJJmdGG2aY\lJJRwKHerbHSgeJlx\Q>? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4N{ezNUc,OjR7Nke3N|E9N2F-
Assay
Methods Test Index PMID
Western blot Cyclin B / PH3 ; AR / PSA ; p-SREBP-1 / N-SREBP-1 / p-SREBP-2 / N-SREBP-2 / FASN / HMGCR 27378817 24493696
Immunofluorescence α-tubulin / centromere 27378817
Growth inhibition assay Cell viability 24493696
In vivo Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake[1]. Fatostatin significantly inhibits subcutaneous C4-2B tumor growth and markedly decreases serum PSA level compared to the control group[2].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: CHO-K1 cells
  • Concentrations: 20 μM
  • Incubation Time: 20 h
  • Method: On day 0, CHO-K1 cells are plated out onto a 96-well plate in medium A. On day 2, the cells are transiently cotransfected with pCMV-PLAP-BP2(513–1141), pCMV-SCAP, and pAc-β-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 β-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of β-galactosidase.
Animal Research:[1]
  • Animal Models: Obese (ob/ob) mice (C57BL/6J background)
  • Dosages: 30 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 7 mg/mL
(18.65 mM)
Water Insoluble
Ethanol ''''''''25 mg/mL warmed

Chemical Information

Molecular Weight 375.33
Formula

C18H18N2S·HBr

CAS No. 298197-04-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NC=CC(=C1)C2=NC(=CS2)C3=CC=C(C=C3)C.Br

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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