TABLE 2.

GEF-interaction inhibitors of Rac and Cdc42 in cancer.

Rac-GEF interaction inhibitors
GEF	Inhibitor	References	IC50	In vivo models
Dock 1	TBOPP	Tajiri et al., 2017	8.4 μM	Lung metastasis mouse model
Dock 1, 2, and 5	CPYPP	Nishikimi et al., 2012	∼ 23 μM	–
Dock 2	Dcpep-3	Sakamoto et al., 2017	12 nM	–
	Dcpep-4	Sakamoto et al., 2017	6 nM	–
	Cholesterol sulfate	Sakurai et al., 2018	2 μM	–
Dock 5	C21	Vives et al., 2011	n.d	Bone metastasis mouse model (Vives et al., 2015)
Fgd5	Aurintricarboxylic acid	Park et al., 2019	157 nM	–
p-Rex	1A-116	Cardama et al., 2014a, b	1–10 μM	Experimental metastasis mouse model
Tiam	ZINC07949036	Ferri et al., 2009	24.1 μM	–
	ZINC08010136	Ferri et al., 2009	12.2 μM	–
	ZINC69391	Cardama et al., 2014a, b	31–61 μM	Breast cancer metastasis mouse model
	K91	Niebel et al., 2013	Kd = 209 nM	–
Tiam 1, Trio, Vav2	Compound 4	Ferri et al., 2013a	8.7 μM	–
Tiam-1, Trio	NSC23766	Gao et al., 2004	50–100 μM	Anaplastic large-cell lymphoma (ALCL)- Mice/xenograft model (Colomba et al., 2011) Chronic myelogenous leukemia mice model (Thomas et al., 2007) Murine orthopic gliobastoma xenograft model (Karpel-Massler et al., 2013)
TrioN	ITX3	Bouquier et al., 2009	50-100 μM	−
Vav	EHop-016	Montalvo-Ortiz et al., 2012	1 μM	Metastatic breast cancer mouse model (Castillo-Pichardo et al., 2014) Myxofibrosarcoma xenografts in mice (Okada et al., 2017)
	Azathioprine	Poppe et al., 2006	n.d	Pancreatic cancer mouse model (Razidlo et al., 2015)
Cdc42-GEF interaction inhibitors
GEF	Inhibitor	References
Dbs	AZA197	Zins et al., 2013	1–10 μM	Xenograft model of colon cancer
	Compound 19	Cummings et al., 2009	∼67 μM	–
Intersectin	CASIN	Peterson et al., 2006	2 μM	Colorectal cancer Mice/xenograft model (Sakamori et al., 2014)
	ZCL278	Friesland et al., 2013	Kd = 11.4 μM	–
	ZLC367	Aguilar et al., 2019	0.098 nM	Xenograft mouse model of lung cancer
PIP-2 mediated GEF activity	Pirl1	Peterson et al., 2006	3 μM	–