TABLE 2

ML120B and PS1145 cellular selectivity assay


Cellular Pathway Selectivity
Reporter
Stimulator
Pathway
IC50 (μM)
ML120B
PS1145
NF-κB PMA IKK/inflammation/apoptosis 2.8 1.7
AP-1 PMA JNK/stress/growth >30 8.8
NFAT PMA + ionomycin PKC and Ca2+/calcineurin >30 6.6
SRE PMA MAPK/ERK/growth >30 >30
CRE Forskolin PKA/stress >30 >30
ISRE IFNβ JAK/STAT/inflammation >30 >30
IL-8 TNFα Inflammation marker (cytokine) 6.3 3.4
ELAM
TNFα
Inflammation marker (selectin)
0.5
0.9
  • NFAT, nuclear factor of activated T cells; SRE, serum response element; CRE, cAMP response element; ISRE, interferon-stimulated response element; IFN, interferon; JNK, c-Jun NH2-terminal kinase; MAPK, mitogen-activated protein kinase; ERK, extracellular signal-regulated kinase; PKA, protein kinase A; JAK, Janus tyrosine kinase; STAT, signal transducer and activator of transcription.