Table 2:

The inhibitors targeting SCAP/SREBPs pathway in cancer cells

Drug	Mechanism	Cancer type	In Vitro Cell line (IC50 μM)	In vivo xenograft mouse model (drug dose)	References
Fatostatin	Inhibition of ER-Golgi translocation of SCAP/SREBPs	GBM	U87-MG (−)	U87-MG (5, 30 mg/kg)	[108]
		Prostate	LNCap(10.4), C4–2B(9.1), PC3 (15.8), DU145 (9.5)	C4–2B, PC3,DU145(15 mg/kg)	[109, 111]
		Lung	A549 (−), PC9 (−)	None	[141]
		Pancreatic	MIA PaCa-2 (14.5)	None	[72]
Betulin	Inhibition of ER-Golgi translocation of SREBPs	Prostate	LNCaP (−), PC3 (−)	None	[142]
		Breast	MCF7 (−)	MCF7 (50,100 mg/kg)	[143]
		Lung	A549 (−), PC9 (−)	A549 (20 mg/kg)	[141]
		HCC	None	Diethylnitrosamine-induced mouse HCC (50 mg/kg)	[138]
Xanthohumol	Inhibition of ER-Golgi translocation of SCAP/SREBPs by binding to Sec23/24	Normal liver	None	75 or 150 mg/kg dietary Xanthohumol inhibits SREBP-1 target gene expression in the liver in diet-induced obese mice	[117]
PF-429242	Inhibition of SREBP cleavage by inhibiting SIP	Normal liver	None	PF-429242 with 10 or 30 mg/kg inhibits the expression of SREBP target genes in mice liver	[126]
		HCC	Huh-7 (90)	None	[144]
		GBM	T98(15.0), U87- MG(15.2), A172 (27.6)	None	[128]
		Pancreatic	MIA PaCa-2 (24.5)	None	[72]
Nelfinavir	Inhibition of SREBP cleavage by inhibiting S2P	Liposarcoma	LiSa-2 (−), SW872 (−)	LiSa-2 (500 mg/kg)	[132]
		Prostate	DU145 (−), PC3 (−)	None	[134]
1,10-phenanthroline	Inhibition of SREBP cleavage by inhibiting S2P	Prostate	DU145 (−), PC3 (−)	None	[134]
BF175	Inhibition of the transcription activity of SREBPs	Normal liver	None	BF175, 0.2% per weight of diet for 8 weeks, decreases the expression of SREBP target genes in mouse liver and reduces hepatic and blood levels of lipids	[137]