Table 3.

Pimozide

Cancer type	Cell line	Model used	Molecular targets	Efficacy	IC50 (μM)	Reference
Breast cancer	MCF-7	In vitro, orthotopic mouse model	Sigma 2 sites, p-STAT5, Ereg, Epgn, Nrg1, Cuzd1	Radiosensitization, Anti-proliferation, Apoptosis, Cell cycle arrest	6	[37, 51, 57, 59]
	T47D, ZR75–1B, MDA-MB-231	In vitro		Anti-proliferation		[37]
Retinoblastoma	Y79 WERI-Rb-1	In vitro	Ca2+ T-channels	Anti-proliferation, Apoptosis, Cell cycle arrest	0.9 1.2	[44]
Rat glioma	C6	In vitro	Ca2+ T-channels	Anti-proliferation, Apoptosis, Cell cycle arrest	8.0	[44]
Glioblastoma	Patient-derived cell lines	In vitro, orthotopic mouse model	Caspase 3, PARP, USP1, ID1, Sox2, Olig2, CHEK1, p-gH2AX	Anti-proliferation, Apoptosis		[61]
Leukemia	K562	In vitro, subcutaneous mouse model	USP1, ID1	Anti-proliferation, Tumor growth inhibition		[62]
Chronic myelogenous leukemia	K562, KU812	In vitro	STAT5, p-STAT5, MAPK, p-MAPK	Apoptosis, Cell cycle arrest		[10]
Acute myelogenous leukemia	MV411 Ba/f3 FLT3 ITD 32D/ITD	In vitro, orthotopic mouse model	p-Tyr STAT5, STAT5, FL3-ITD, PI3K, Akt, mTOR, 4EBP1, Mcl-1	Anti-proliferation, Apoptosis, Tumor growth inhibition	3–5	[49] [50]
T-cell leukemia/lymphoma	Ba/F3 Kit225 HuT102	In vitro	p-STAT5, STAT5, TRAIL/DR4	Anti-proliferation, Apoptosis	15 11	[53] [54] [55]
Lung cancer	NSCLC A549, H460, HCC4006, H1437, H520	In vitro	USP1	Anti-proliferation		[47] [67]
	H322, SKLU-1, SW1573, H522, H1299, H1703,				5.0–13.7
Hepatocellular carcinoma	MHCC-97L Hep 3B Hep G2 Huh7	In vitro, subcutaneous mouse model (MHCC-97L only)	Bmi1, c-Myc, Nanog, STAT3, IL-6, N-cadherin, vimentin, E-cadherin, wnt/β-catenin, EpCAM, cyclin D1, PKA, GSK3	Anti-proliferation, Cell cycle arrest, Anti-invasion, Tumor growth inhibition	6.15 1.81 1.14 8.44	[35, 45]
Osteosarcoma	U2OS	In vitro	ERK, PARP, STAT3, catalase, ROS	Anti-proliferation, Apoptosis, Cell cycle arrest	13.78	[5]
Prostate cancer	DU145 LNCaP PC3M BPH-1 22RV1	In vitro	p-Tyr705 STAT3, STAT3, STAT5A, IL-6, N-cadherin, E-cadherin	Anti-proliferation, Apoptosis, Cell cycle arrest, Anti-invasion	6.541 7.21 9.19 7.78 11.12	[39] [40]
Pancreatic cancer	K562, Panc-1 MiaPaCa2 BxPC-3	In vitro, orthotopic mouse model	Caspase 3/7, DRD2, p-STAT5, p-ERK, PKA, ER stress	Anti-proliferation, Apoptosis, Tumor growth inhibition	5	[58] [52]