Table 1.
Effect on cyst formation
|
||||
---|---|---|---|---|
Inhibitor | Conc.(μM) | Pathway affected | WT SYT | SYTdl 1–40 |
Untreated | ----- | ----- | None | None |
DMSO | ----- | ----- | None | None |
Genestein | 40 | Tyrosine kinase CFTR | Complete inhibition | Complete inhibition |
AG1478 | 10 | EGFR | None | None |
Reactive Blue 2 | 500 | P2YR | Complete inhibition | Complete inhibition |
PPADS | 500 | P2YR | Profound inhibition† | Profound inhibition |
NF023 | 50 | P2XR | None | None |
LY290042 | 10 | PI3K | Reduced Growtha | Reduced Growth |
H-89 | 10 | PKA | None | None |
Calphostin | 2.5 | PKC | None | None |
W-7 | 50 | Calcium | None | None |
PD98069 | 50 | MEK1 | Complete inhibition | Complete inhibition |
SP600125 | 50 | JNK | Complete inhibition | Complete inhibition |
SB220025 | 50 | p38MAPK | Complete inhibition | Complete inhibition |
Rac Inhibitor | 50 | Rac1 | Complete inhibition | Complete inhibition |
reduced growth signifies that the size of the individual MDCK cysts was around half the size of the untreated control. Bolded names designate P2YR specific inhibitors.
Profound inhibition implies a very significant reduction in the number of intact cysts caused by the PPADS inhibitor. The reduction is quantitated in Table 2.