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Fatostatin (hydrobromide)

Item № 13562
CAS № 298197-04-3
Purity ≥95%
product image
                (CAS 298197-04-3)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $55.00 0.00
     10 mg $77.00 0.00
     25 mg $138.00 0.00
     50 mg $248.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

Description
Synonyms
  • 125B11

Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.1 The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.2 Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).3,4 This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.3 Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).5 Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.6 This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.3

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Technical Information
Formal Name
4-[4-(4-methylphenyl)-2-thiazolyl]-2-propyl-pyridine, hydrobromide
CAS Number
298197-04-3
Synonyms
  • 125B11
Molecular Formula
C18H18N2S • HBr
Formula Weight
375.3
Purity
≥95%
Formulation
A crystalline solid
λmax
257, 336 nm
SMILES
CC(C=C1)=CC=C1C2=CSC(C3=CC(CCC)=NC=C3)=N2.Br
InChI Code
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Horton, J.D., Goldstein, J.L., and Brown, M.S. SREBPs: Activators of the complete program of cholesterol and fatty acid synthesis in the liver Journal of Clinical Investigation 109, 1125-1131 (2002).

2. Raghow, R., Yellaturu, C., Deng, X., et al. SREBPs: The crossroad of physiological and pathological lipid homeostasis Trends in Endocrinology and Metabolism 19(2), 65-73 (2008).

3. Kamisuki, S., Mao, Q., Abu-Elheiga, L., et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP Chemistry & Biology 16, 882-892 (2009).

4. Kamisuki, S., Shirakawa, T., Kugimiya, A., et al. Synthesis and evaluation of diaryl thiazole derivatives that inhibit activation of sterol regulatory element-binding proteins Journal of Medicinal Chemistry 54(13), 4923-4927 (2011).

5. Choi, Y., Kawazoe, Y., Murakami, K., et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds The Journal of Biological Chemisty 278(9), 7320-7324 (2003).

6. Uttarwar, L., Gao, B., Ingram, A.J., et al. SREBP-1 activation by glucose mediates TGF-ß upregulation in mesangial cells American Journal of Physiology.Renal Physiology 302(3), F329-F341 (2012).

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