Table 2.
Summary of hNek6 variants thermal shift inhibitor screen. A thermal shift of at least 2 °C (ΔTm ≥ 2 °C) is depicted in italics and a significant thermal shift (ΔTm > 4 °C) is depicted in bold. (D: dephosphorylated).
CompoundDescription | Nek6wt | Nek6wtD | Nek6(S206A) | Nek6(S206A)D | Nek6(Δ1-44) |
---|---|---|---|---|---|
Alsterpaullone | 0.0 | 0.1 | 1.4 | 2.9 | −0.5 |
Alsterpaullone, 2-Cyanoethyl | 0.0 | −0.1 | 2.5 | 2.5 | −0.2 |
Aminopurvalanol A | 0.3 | −1.8 | 0.8 | _ | −0.2 |
Aminopyrazole1 | −0.4 | 0.1 | 1.0 | 2.4 | 0.0 |
AR-A014418 | 0.3 | −0.5 | 1.4 | 2.6 | −0.2 |
Indolinone1 | _ | −0.4 | −0.2 | 2.1 | −0.5 |
Indolocarbazole1 | −0.3 | −0.1 | 1.7 | 0.7 | −1.3 |
Isogranulatimide | 1.2 | 0.6 | 6.5 | 2.3 | −0.7 |
JNJ-7706621 | 0.0 | 0.6 | 0.7 | 2.1 | −0.7 |
Pyrazolanthrone | 0.3 | −1.1 | 1.8 | 2.3 | 0.1 |
Staurosporine | 0.3 | −0.7 | 2.1 | 2.3 | _ |
TPCA-1 | 0.0 | −0.7 | 0.9 | 2.0 | −1.7 |