Table 1.

Summary of kinase-inhibitors and their effects on bioluminescent TGFBR1 reporter activity and phosphorylated Smad2 levels

Kinase- inhibitors (10µM)	Reporter bioluminescence (Fold response)		1833 (Fold response)	pSmad2 levels	Kinase-inhibitor target(s)*	References: inhibitors and C-terminal pSmad2/3
	BTR- WT	BTR- MUT	BTR- WT
Vehicle (DMSO)	1.0	1.0	1	0.0
TGFβ only	0.4	1.0	-	1.0
SB431542	10.0	2.0	3.9	0.0	TGFBR1 kinase	(21, 22, 41, 50)
PP2	4.0	1.0	4.1	0.1	Src family non-receptor tyrosine kinases	(25)
AG1478	8.2	0.9	12.7	0.1	PTK inhibitor selective for EGFR	(37)
AG825	3.6	0.9	0.89	1.1	PTK inhibitor selective for EGFR	(37)
SP600125	4.8	1.2	16.8	0.8	c-Jun N-terminal kinase (JNK)	(41, 42, 45)
SB203580	8.0	1.1	4.0	0.7	p38 MAP kinase activity	(41, 42, 44)
SB202190	6.2	0.8	6.4	0.5	p38 MAP Kinase	(43)
BML257	5.0	1.1	3.1	1.1	Akt1/2/3 serine-threonine protein kinases
Staurosporine	3.0	0.5	4.2	0.6	Pan-specific	(32)
LY294002	5.4	0.8	12.3	0.1	Phosphoinositide 3-kinase (PI3K)	(41, 47)
Quercetin	4.6	1.1	2.0	1.0	EGFR and Her-2 tyrosine kinase, PI3K,	(34)
Erlotinib	n/a	n/a	n/a	0.6	EGFR tyrosine kinase	(37)
Lapatinib	n/a	n/a	n/a	0.0	EGFR and Her-2 tyrosine kinase	(37)

^*target information from product inserts