- Cat. No.
- A11230
PF 429242
PF 429242 is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease.
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SREBP inhibitors block the transcription factors that switch on cholesterol and fatty acid synthesis. Sterol regulatory element-binding proteins (SREBPs) are made as inactive precursors in the endoplasmic reticulum (ER) membrane. When sterol levels fall, SREBP cleavage-activating protein (SCAP) escorts them to the Golgi, where two proteases release the active transcription factor. A 1997 review described this pathway as regulated proteolysis of a membrane-bound transcription factor. PF 429242 inhibits site-1 protease and was shown in 2008 to reduce SREBP processing and lipid synthesis. Fatostatin, reported in 2009, blocks SREBP activation and fat synthesis in cells. SREBP/SCAP-IN-1 and 4'-hydroxyflavanone are listed as further inhibitors of SREBP maturation in cells.
PF 429242 is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease.
Synonyms: PF 429242
PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.
Synonyms: Fatostatin A
Fatostatin Hydrobromide is an inhibitor of sterol regulatory element-binding protein (SREBP).
Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.
FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
Synonyms: 125B11
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2.
Pseudoprotodioscin is a furostanoside that inhibits Sterol Regulatory Element-Binding Proteins (SREBPs) and microRNA 33a/b. This inhibition leads to a reduction in the gene expression involved in cholesterol and triglyceride synthesis. Pseudoprotodioscin is valuable for research on lipid metabolism and related cardiovascular diseases.
4'-Hydroxyflavanone is an inhibitor of SREBP maturation, impacting lipid synthesis. As a synthetic analogue of flavanone, it demonstrates potential in studies related to hepatic steatosis and dyslipidemia. This compound can be utilized to explore mechanisms of lipid metabolism and associated disorders.
SREBP/SCAP-IN-1 is a selective inhibitor of the SREBP/SCAP complex, which plays a crucial role in lipid metabolism and cellular cholesterol homeostasis. This compound effectively disrupts the signaling pathway involved in sterol regulatory element-binding protein activation, providing insight into lipid regulation mechanisms. Research applications include investigating metabolic disorders, cardiovascular diseases, and potential therapeutic strategies targeting cholesterol metabolism.
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SREBP/SCAP-IN-2 is a selective inhibitor of the SREBP/SCAP complex, which plays a crucial role in lipid metabolism and cellular cholesterol homeostasis. This compound effectively interferes with the activation and function of SREBP, thereby modulating lipid biosynthesis pathways. SREBP/SCAP-IN-2 is valuable for research focusing on metabolic disorders, obesity, and cardiovascular diseases, providing insights into the regulatory mechanisms of lipid metabolism.
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