A novel p38α MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model

Table 1 MW01-2-069A-SRM selectivity in standard kinase profiling screen

Kinase	% kinase activity	Kinase	% kinase activity	Kinase	% kinase activity	Kinase	% kinase activity
ASK1	107	IRAK4	112	MLK1	94	PKBβ	91
CDK1/cyclinB	94	JAK2	108	MSK1	94	PKBγ	100
CDK2/cyclinA	94	JNK1α 1	90	MSK2	96	PRAK	86
CDK5/p25	90	Lyn	94	p70S6K	111	Pyk2	83
CK2	96	ERK1	90	p38α	-2	ROCK-I	89
FAK	96	ERK2	99	p38β	30	RSK1	100
Fyn	98	MAPKAP-K2	97	p38δ	101	Syk	96
GSK3β	74	MAPKAP-K3	94	p38γ	95	TAK1	97
IKKα	95	MEK1	104	PAK2	116	TAO1	94
IKKβ	104	MKK4	117	PDK1	101	TAO2	92
IRAK1	110	MKK7β	103	PKBα	76	TBK1	95

The ability of 069A (20 μM final concentration of compound; 90 μM final concentration of ATP) to suppress the activity of purified kinases was determined in a Millipore/Upstate kinase profiling assay as described by the manufacturer. Kinase activity in the absence of inhibitor is taken as 100%.

ISSN: 1742-2094