Identification of hematein as a novel inhibitor of protein kinase CK2 from a natural product library

BMC Cancer

Table 1 Specificity spectrum of hematein.

Protein kinase	Kinase activity (%)	Protein kinase	Kinase activity (%)
Abl	76	Lyn	111
CDK1	95	MAPK1	87
CDK2	113	MAPK2	74
CDK3	55	MKK6	99
CDK5	84	MSK1	91
CDK7	106	MSK2	72
CHK1	65	mTOR	103
CK1	82	p70S6K	61
CK2	0	PDGFRα	103
cKit	83	PDK1	96
c-RAF	102	Pim-1	58
cSRC	94	Pim-2	81
DRAK1	51	Pim-3	50
DYRK2	91	PKA	95
EGFR	31	PKBα	92
Flt1	31	PKCα	36
Flt3	83	PKD2	58
GCK	94	PRAK	65
GSK3β	147	ROCK-II	75
HIPK1	94	SAPK2a	121
HIPK2	76	SAPK3	99
HIPK3	96	SAPK4	112
KDR	62	SGK	92
Lck	113	Syk	136

Residual activity is determined in the presence of 10 μM hematein under 10 μM ATP and expressed as a percentage of the control without inhibitor. Residual activities ≤ 10% are shown in bold. CDK, cyclin-dependent kinase; CHK, checkpoint kinase; CK, casein kinase; SRC, sarcoma kinase; DRAK, DAP kinase-related apoptosis-inducing protein kinase; DYRK, dual-specificity tyrosine-(Y)-phosphorylation regulated kinase; EGFR, epidermal growth factor receptor; Flt, fms-related tyrosine kinase; GCK, gluokinase; GSK, glycogen synthase kinase; HIPK, homeodomain interacting protein kinase; KDR, kinase insert domain receptor; Lck, lymphocyte cell-specific protein-tyrosine kinase; MAPK, mitogen-activated protein kinase; MKK, mitogen-activated kinase; MSK, mitogen- and stress-activated protein kinase; mTOR, mammalian target of rapamyin; p70S6K, p70 S6 kinase; PDGFR, platelet-derived growth factor receptor; PDK, 3'-phosphoinositide-dependent kinase; PKA, protein kinase A; PKB, protein kinase B; PKC, protein kinase C; PKD, protein kinase D; PRAK, p38-regulated activated kinase; ROCK, Rho-dependent protein kinase; SRPK, serine-arginine protein kinase; SGK, serum and glucocorticoid-inducible kinase.

ISSN: 1471-2407