Kinase probes


Target Probe Control Targeted domain Mode of action Recommended concentration Target origin
BUB1 BAY 1816032 BAY-283 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 300 nM human
PIP4K2A BAY-091 BAY-0361 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 - 10 µM human
PRKAA1, RPS6KA1 BAY-3827 BAY-974 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 150 nM human
MET BAY-474 BAY-827 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 0.001 - 1 µM human
ROCK1, ROCK2 BAY-549 BAY-4900 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 100 nM human
TIE1, TEK, DDR1, DDR2 BAY-826 BAY-309 Kinase domain (active site) Inhibitor (type 2, ATP competitive) ≤ 0.5 µM human
MAPK7 BAY-885 BAY-693 Kinase domain (active site) Inhibitor (type 1.5, ATP competitive) 1 µM human
TBK1, IKBKE BAY-985 BAY-440 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
AKT1, AKT2, AKT3 BAY1125976 BAY-940 Kinase domain (allosteric pocket) Covalent inhibitor (type 4, non-ATP competitive) ≤ 1 µM human
IKBKB BI 605906 BI-5026 Kinase domain (active site) Inhibitor (ATP competitive) ≤ 5 µM human
CIT C3TD879 C3TD879-N Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 2 µM human
SGK3 SGK3-PROTAC1 cisSGK3-PROTAC1 Kinase domain (active site) PROTAC degrader (ATP competitive) ≤ 3 µM human
MAPK14 FS-694 FM-743 Kinase domain (active site) Inhibitor (type 1.5, ATP competitive) 0.1 - 1 µM human
IRAK4 GNE-2256 GNE-6689 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
LIMK1 SM311 SM311-NC Active site (covalent binding to Cys349) Covalent inhibitor 0.1 -1 µM human
LIMK2 THNAN69 THNAN69-NC ATP binding pocket Degrader 10 - 100 nM human
CDK7 JNJ-3738 JNJ-6240 Kinase domain (active site) Covalent inhibtor (ATP competitive) ≤ 1 µM human
CSNK1D, CSNK1E JNJ-6204 JNJ-0293 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
MAPK3, MAPK1 ERKi ERKi-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
LRRK2 MLi-2 MLi-2-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
SYK MRL-SYKi MRL-SYKi-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) 100 nM human
PTK2, PTK2B PF-04554878 PF-00911705 Kinase domain (active site) Inhibitor (ATP mimetic) 100 nM human
DDR1, DDR2, MAPK11, MAPK14 SR-302 SR-301 Kinase domain (active site) Inhibitor (type 2, ATP competitive) 100 nM human
MAPK14 SR-318 SR-321 Kinase domain (active site) Inhibitor (type 2, ATP competitive) < 100 nM human
MAPK14 Skepinone-L FM-743 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
panCLK (CLK1, CLK2, CLK3, CLK4) T3-CLK T3-CLK-N Kinase domain (active site) Inhibitor (type 1, ATP competitive) < 100 nM human
ACVR1B, TGFBR1 TP-008 Al11 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 - 10 µM human
RIPK1 TP-030-1 TP-030n Kinase domain (allosteric pocket) Inhibitor (type 3, non-ATP competitive) 100 nM human
RIPK1 TP-030-2 TP-030n Kinase domain (allosteric pocket) Inhibitor (type 3, non-ATP competitive) 100 nM human
AKT1, AKT2, AKT3 Borussertib RL2578 Kinase domain (allosteric pocket) Covalent inhibtor (type 4, non-ATP competitive) 1 µM human