Substrates & Inhibitors
Our collection of enzyme substrates and inhibitors gives you access to the essential tools to build your own assay. The assay development expertise behind KinaseProfiler™ is now available to you - choose the enzyme target and browse through a list of relevant substrates or inhibitors.
| Inhibitor | Catalogue Number | Kinase | IC50 |
| HA1077 | 19-164 | Rhoa/ROCK-II PRK2 MSK1 Rsk2/MAPKAP-K1b | 2 µM 4 µM 5 µM 15 µM |
| H89 | 19-141 | S6 Kinase 1 MSK1 PKA Rhoa /ROCK-II Akt1/PKBa Rsk2/MAPKAP-K1b | 80 nM 120 nM 50-140 nM 270 nM 2.6 mM 2.8 mM |
| Rottlerin | 19-162 | PRAK MAPKAP-K2 5. PKCd | 1.9 mM 4 µM 3-6 µM |
| U0126 | 19-147 | MEK1/MEK2 MKK1 PRAK p38/SAPK2a Akt1/PKBa | 100 nM 13 µM 50 µM 55 µM 60 µM |
| SB 202190 | 19-134 | p38a/SAPK2a p38a/SAPK2b | 50-280 nM 100-350 nM |
| LY 294002 | 19-142 | PI3 Kinase Casein Kinase 2 | 1.4-10 µM 6.9 µM |
| Ro 318220 | 19-163 | Rsk2/MAPKAP-K1b MSK1 | 3 nM 8 nM |
| HA1077 | 19-164 | ROKa/ROCK II PRK2 MSK1 Rsk2 PKA, p70 S6 Kinase, CaM Kinase MLCK | 1.9 µM 4 µM 5 µM 15 µM (K i = 1.8nM) (K i = 1.8nM) |
| PD 184352 | 19-166 (note: does not inhibit other protein kinases at 10 µM | MEK1 | 300nM in vitro 2nM in vivo |
| Raf1 Kinase Inhibitor | 19-167</a> | cRAF1 | 9 nM |
(Shows ³ 100-fold selectivity for Raf kinase versus Cdk1, Cdk2, c-sr c , ERK2, MEK, p38, Tie2, VEGFR2 and c-fms).
*Data from Davies, S.P., et al., Biochem. J. 351: 95, 2000
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