Table 1. Ciliation phenotypes of kinase inhibitor target proteins depleted by siRNAs.
IC50 values are derived from sources noted in Table 1, or were described by Anastassiadis et al.(27)
| siRNA | Compound (activity against the protein target) | Effect on the primary cilium |
|---|---|---|
| CAMKK2 | SB218078 (7.93), SU11652 (48) | No |
| CHEK1 | Sunitinib (29.2), SB218078 (3.63), SU11652 (15.15) | Stabilization |
| EGFR | Erlotinib (4.21), PD174265 (2.17) | Stabilization |
| FGFR1 | SB218078 (29.13), SU11652 (20.28) | No |
| FLT3 | Sunitinib (2.71), SB218078 (0.19), VEGFR2 inhib. II (3.86), SU11652 (0.78), VEGFR2 inhib. I (13.31) | No |
| GSK3A | GSK-3b Inhibitor XI (8.56), SB218078 (2.19) | Destabilization |
| GSK3B | GSK-3b Inhibitor XI (25.18) | Destabilization |
| IRAK1 | IRAK¼ Inhibitor (15.03) | No |
| IRAK4 | IRAK¼ Inhibitor (22.83) | Stabilization |
| KDR/VEGFR2 | Sunitinib (28.67), SB218078 (4.55), SU11652 (13.76) | No |
| KIT | Sunitinib (8.74), VEGFR2 inhib. II (30.49), SU11652 (28.74), VEGFR2 inib. I (46.29) | No |
| LRRK2 | Sunitinib (3.34), SB218078 (1.91), VEGFR2 inhib. II (7.03), SU11652 (1.44), VEGFR2 inhib. I (28.59) | Destabilization |
| LYN | Sunitinib (23), SB218078 (35.38), SU11652 (6.34) | No |
| MAP2K1 | MEK1/2 inhibitor (IC50=180 nM) | No |
| MAP2K2 | MEK1/2 inhibitor (IC50=220 nM) | Stabilization |
| MARK1 | Sunitinib (40.94), SB218078 (10.43), SU11652 (18.07) | No |
| MERTK | Sunitinib (39.82), SB218078 (13.63), SU11652 (11.5) | Stabilization |
| NUAK1 | Sunitinib (2.75), SB218087 (2.09), VEGFR2 ihnib. II (27.73), SU11652 (2.06) | No |
| PDGFRA | Sunitinib (10.85), SB218078 (32.83), SU11652 (25.86) | Destabilization |
| PDGFRB | Sunitinib (17.64), SU11652 (9.28) | Destabilization |
| PIK3CB | DNA-PK Inhibitor III (IC50=135 nM) | Stabilization |
| PRKDC | DNA-PK Inhibitor III (IC50=120 nM) | Stabilization |
| PTK2 | Sunitinib (27), SB218078 (23.48), SU11652 (25.84) | No |
| RET | Sunitinib (3.43), SB218078 (3.21), VEGFR2 inhib. II (42.87), SU11652 (2.47), VEGFR2 inhib. I (40.82) | No |
| SRC | Sunitinib (39.81), SU11652 (26.02) | No |
| YES1 | Sunitinib (5.91), SB218078 (31.86), SU11652 (5.29) | No |