SB204990 (SB) is a specific inhibitor of the ATP-citrate lyase (ACLY) enzyme, leading to a reduction in cytosolic Ac-CoA levels and consequently expected to diminish levels of acetylated and active β-catenin[1].
体内研究
Oral administration of SB 204990 to rats is effectively absorbed into the systemic circulation, and its inclusion in the diet (0.05-0.25%, w/w) for one week results in a dose-related decrease in plasma cholesterol (up to 46%) and triglyceride levels (up to 80%). In dogs, SB 204990 (25 mg/kg per day) also reduces plasma cholesterol (up to 23%) and triglyceride levels (up to 38%), with a preference for lowering low-density lipoprotein cholesterol compared to high-density lipoprotein cholesterol levels[2].
体外研究
SB204990 (SB) is a specific inhibitor of the ATP-citrate lyase (ACLY) enzyme, leading to a reduction in cytosolic Ac-CoA levels and consequently expected to diminish levels of acetylated and active β-catenin[1].
SB 204990 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Hep G2 cells
30 µM
2.5 hours
Inhibited cholesterol and fatty acid synthesis by 91% and 82% respectively
Biochem J. 1998 Aug 15;334 ( Pt 1)(Pt 1):113-9
A2780/CDDP
30 µM
24, 48, or 72 hours
SB-204990 synergized with cisplatin to reduce IC50 values
Front Oncol. 2021 Mar 17;11:642229
Pkd1-null collecting duct cells (ID1-3E5)
30 µM
3 days
Inhibited cystic growth, SB-204990 significantly reduced cyst area
Front Mol Biosci. 2022 Nov 25;9:1001941.
Pkd1-null proximal tubule cells (PN24)
30 µM
3 days
Inhibited cystic growth, SB-204990 significantly reduced cyst area
Front Mol Biosci. 2022 Nov 25;9:1001941.
SB 204990 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c male athymic nude mice
Subcutaneous xenograft tumor model
Intraperitoneal injection
135 mg/kg
Once daily for 14 days
SB-204990 greatly abolished the promoting effect of CUL3 knockdown on xenograft tumor growth
Genes Dev. 2016 Sep 1;30(17):1956-70
Rats
Sprague-Dawley rats
Intravenous injection
150 µmol/kg
Two injections, 245 and 65 minutes apart
Inhibited hepatic cholesterol and fatty acid synthesis by 76% and 39% respectively
Biochem J. 1998 Aug 15;334 ( Pt 1)(Pt 1):113-9
Nude mice
Ovarian cancer xenograft model
Intraperitoneal injection
4 mg/kg
Days 7, 14, and 28, three times in total
ACLY knockdown synergized with cisplatin to inhibit tumor growth
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