GW296115

GW296115 (1 μM) inhibits 25 out of 403 wild-type human kinases by over 90% at a concentration of 1 μM, with a selectivity index of 0.062^[1].
GW296115 potently inhibits 6 IDG dark kinases in enzymatic assays, with IC₅₀ values ranging from 5.5 nM (DRAK2) to 89 nM (DCAMKL3)^[1].
GW296115 (1 μM; 72 h) exerts no effect on cell proliferation in 17 tested cancer cell lines and normal cell lines (including non-malignant MCF10A and MRC-5) following treatment at 1 μM for 72 h^[1].
GW296115 (incubated for 2 h) potently binds to BRSK2 in living HEK293 cells with an IC₅₀ of 107 nM, confirming that it is a cell-active BRSK2 inhibitor^[1].
GW296115 (2.5 μM; 2-6 h) abolishes BRSK2-induced phosphorylation of AMPK substrates in HEK293T cells (this effect is observed at both 2 h and 6 h) and induces hyperphosphorylation of BRSK2 at the T174 site^[1].
GW296115 (2-5 μM) inhibits autophagy and enhances apoptosis in MDA-MB-231 triple-negative breast cancer cells, while it also inhibits autophagy and enhances apoptosis in BT-474 estrogen receptor-positive breast cancer cells^[2].
GW296115 (2 μM; 24 h) inhibits the growth of MDA-MB-231 triple-negative breast cancer cells^[2].
GW296115 (2-3 μM; 72 h) reduces the 3D invasiveness of MDA-MB-231 triple-negative breast cancer cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.