Table 1. IC50 values for small molecule inhibitors of TGF–β1 signaling.
| Compound name | Activity | Impedance IC50 [nM] |
MS / MS α–SMA IC50 [nM] |
MS / MS COL1 IC50 [nM] |
HCA IC50 [nM] |
|---|---|---|---|---|---|
| EW–7197 | ALK5 inhibitor | 47±25 (n = 7) | 51±17 (n = 7) | 110±30 (n = 7) | 80±30 (n = 7) |
| SB525334 | ALK5 (4) inhibitor | 120±25 (n = 2) | 90±5 (n = 2) | 380±110 (n = 2) | 2,500±1,200 (n = 2) |
| Halofuginone | p–SMAD–3 inhibitor | 96±10 (n = 2) | 27±4 (n = 2) | 27±1 (n = 2) | 690±320 (n = 2) |
| 5Z–7–Oxozeaenol | TAK1 inhibitor | 250±170 (n = 3) | 300±270 (n = 3) | 460±270 (n = 3) | 2,600±2,500 (n = 2) |
| Salinomycin | TAK1/p38 pathway inhibitor | 1,500±1,500 (n = 2) | 290±300 (n = 2) | 1,200±1,500 (n = 2) | 15,800 (n = 1) |
| SP600125 | JNK1/2/3 inhibitor | 48,500±2,100 (n = 2) | 38,000±17,000 (n = 2) | 36,000±18,000 (n = 2) | >46,000± (n = 2) |
| L–skepinone | p38 inhibitor | 5,000±49 (n = 2) | 960±440 (n = 2) | 1,500 (n = 1) | 23,000 (n = 1) |
| BX–912 | PDK1 inhibitor | 7,500±1,600 (n = 3) | 8,600±9,400 (n = 3) | 8,700±3,000 (n = 2) | 17,000±6,700 (n = 2) |
| GSK–269962 | ROCK1/2 inhibitor | 1,010±300 (n = 3) | 22±1 (n = 2) | 3,100±92 (n = 2) | 240±270 (n = 2) |
| RKI 1447 | ROCK1/2 inhibitor | 8,400±42 (n = 2) | 150±22 (n = 2) | 12,200±2,400 (n = 2) | 4,300±2,300 (n = 2) |
| BIX 02189 | ERK5 inhibitor | 6,000 (n = 1) | 14,000 (n = 1) | 6,500 (n = 1) | 22,000±11,000 (n = 2) |
| XMD 8–92 | ERK5 inhibitor | 4,400 (n = 1) | 2,400 (n = 1) | 5,400 (n = 1) | 12,000 (n = 1) |
| FR180204 | ERK1/2 inhibitor | 50,000 (n = 1) | 49,000 (n = 1) | 36,000 (n = 1) | >46,000 (n = 1) |
| PD98059 | MEK inhibitor | 19,000 (n = 1) | 50,000 (n = 1) | >50,000 (n = 1) | >46,000 (n = 1) |
| Pamapimod | p38 inhibitor | 19,000 (n = 1) | 34,000 (n = 1) | >50,000 (n = 1) | >46,000 (n = 1) |
| Ipatasertib | AKT1 / 2 / 3 inhibitor | 43,000 (n = 1) | 25,000 (n = 1) | >50,000 (n = 1) | 22,000 (n = 1) |
| EHT 1865 | RAC inhibitor | 14,000 (n = 1) | 16,000 (n = 1) | 28,000 (n = 1) | not assessed |
| LY294002 | PI3K a/d/b inhibitor | 13,000 (n = 1) | 27,000 (n = 1) | 45,000 (n = 1) | 2,400 (n = 1) |
| IC–87114 | PI3K g / d inhibitor | >5,000 (n = 1) | >5,000 (n = 1) | 4,900 (n = 1) | 44,000 (n = 1) |
| Csn–B | NR4A1 agonist (nuclear receptor) | >50,000 (n = 1) | >50,000 (n = 1) | >50,000 (n = 1) | 39,000 (n = 1) |
Values represent mean ± SD; n, number of independent experiments.