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JNJ-17203212 is a selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
LY2409881 3HCl is a selective inhibitor of IKK2 with IC50 of 30 nM and IC50 for IKK1 and other common kinases is at least one log higher.
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively, showing no inhibitory activities against 250 other protein kinases observed.
Panobinostat is a broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay.
Pexidartinib is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with IC50s of 20, 10, and 160 nM in vitro, respectively.
Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM and inactive to PKCζ.
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM and is selective(1000-fold more) against all other isozymes except HDAC8(57-fold more).
Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits > 200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Organic synthesis
AM095 free acid is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
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