Table 2.

Published data obtained with BML-241/CAY10444.

System	Effect	Concentration	Inferred significance	Validation	Conflicting data/caveat	Reference
Transfected HeLa cells	[Ca2+]i increase	10 μM	Blocks S1P3 receptors	No effect on S1P1-Hela		Koide et al. (2002)
Endothelial cells	Expression of adhesion molecules	1–10 μM	S1P3 receptors modulate adhesion molecule expression	Antisense oligonucleotides		Kimura et al. (2006)
Pancreatic Islet β Cells	Cell survival	10 μM	S1P3 receptors mediate protective effects on β-cells against cytokine-induced apoptosis.	None		Laychock et al. (2006)
B lymphocytes	Rap1 activation	10 μM	S1P3 receptors activate Rap1 and might promote B-cell adhesion and migration	None		Durand et al. (2006)
Transfected CHO cells	[Ca2+]i increase	10 μM	BML-241 is not selective			Jongsma et al. (2006)
Astrocytes	Cell migration	10 μM	No role of S1P3	none		Sato et al. (2007)
Fibroblast-like synoviocytes	Cell migration Cytokine/chemokine secretion Cell survival	5 μM	S1P stimulates FLS migration through S1P1 and S1P3, induces cytokine/chemokine secretion through S1P2 and S1P3, and protects from cell apoptosis via S1P1.	None		Zhao et al. (2008)
Multiple myeloma cells	Cell survival	10 μM	S1P3 receptors mediate S1P-induced STAT3 phosphorylation and Mcl-1 upregulation	None		Li et al. (2008b)
Keratinocytes	[Ca2+]i increase	50 μM	S1P3 receptors mediate [Ca2+]i increase	No effect of SEW2871 (S1P1 agonist), inhibition by VPC23019	Specificity of SEW2871 and VPC23019 non-fully characterized	Lichte et al. (2008)
Transfected HEK-293 cells	[Ca2+]i increase	50 μM	S1P3 receptors mediate [Ca2+]i increase	No effect of SEW2871 (S1P1 agonist), inhibition by VPC23019	Specificity of SEW2871 and VPC23019 non-fully characterized	Lichte et al. (2008)
Mouse cardiomyocytes	Erk activation	0.1–10 μM	No role of S1P3	none		Tao et al. (2009)
B35 neuroblastoma cells	Cell migration	10 μM	No role of S1P3	No effect with other S1P3 antagonists (VPC23019, VPC25239)		Hans et al. (2009)
Embryonic stem cells	Erk activation	1–10 μM	S1P5, not S1P3, activate Erk1/2	None		Rodgers et al. (2009)
Tango EDG3 cell lines	GPCR β-arrestin recruitment and deactivation	1 nM–0.1 mM	The EDG3 response to S1P is inhibited by CAY-10444 with an IC50 of 4.6 μM	None		Wetter et al. (2009)
Bronchial smooth muscle	Contractility	10 μM	No role of S1P3	none		Chiba et al. (2010)
Granulosa lutein cells	Cell migration	1 μM	S1P3 receptors are involved in FF-HDL- and S1P-stimulated granulosa cell migration	Effect of suramin	Suramin is non-specific	Becker et al. (2010)
Mouse cardiomyocytes	Cell viability	10 μM	S1P3 receptors play a role in Akt activation and cardiomyocyte viability	none		Tao et al. (2010)
Coronary artery	Vasorelaxation	10 μM	S1P3 receptors mediate endothelium dependent coronary relaxation	No effect of W146 (S1P1 antagonist), but inhibition by VPC23019 (mixed S1P1/S1P3 antagonist)	Specificity of VPC23019 not fully characterized	Mair et al. (2010)
Immature B lymphocytes	Cell migration	100 μM	S1P3 receptors are responsible for immature B-cell chemotaxis to S1P	${\text{S1P}}_3^{-/-}$ immature B-cells unable to migrate to S1P		Donovan et al. (2010)
Estrogen receptor-positive breast cancer cells	Cell migration	10 μM	S1P3 stimulates the accumulation of phosphor-ERK-1/2 and promotes cell migration	siRNA knockdown		Long et al. (2010)
Ovarian cancer cells	Cell proliferation and survival	1 μM	S1P3 receptors do not play a role in cell proliferation and survival	None		Illuzzi et al. (2010)
Mesenteric venules	Microvessel permeability	10 μM	S1P3 receptors do not play a role in the protection by S1P of PAF-induced permeability	None		Zhang et al. (2010)