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Table 1 Effect of cucurbitacin B (CuB) on protein kinase activities in a high-throughput screening

From: Identification and characterization of the Cucurbitacins, a novel class of small-molecule inhibitors of Tropomyosin receptor kinase a

Kinase

Remaining activity(%)

Kinase

Remaining activity(%)

Kinase

Remaining activity(%)

 

Remaining activity(%)

TrkA

5.2±0.8

BRSK2

74.9±1.6

HIPK3

91.3±4.0

PHK

106.4±8.4

CAMK1

12.9±3.7

ERK5

75.1±10.6

PKD1

91.6± 11.2

IRAK4

107.5±9.8

AMPK

22.6±1.5

MKK1

75.7±3.8

TIE2

92.2±2.5

p38d MAPK

108.1±21.4

Aurora B

23.2±2.8

IKKb

76.5±18.1

BRSK1

93.3±2.0

CK2

108.3±32.0

YES1

29.8±3.7

MAPK-K3

77.2±1.4

MNK1

94.2±15.4

ERK2

108.5±14.9

TSSK1

33.8±5.0

MLK3

77.4±13.5

ROCK 2

94.8±3.4

DAPK1

108.5±18.5

PIM3

40.6±5.2

SmMLCK

77.4±10.9

PKBa

94.9±14.1

PRK2

108.7±14.7

PAK4

42.3±4.6

CK1Îł2

77.6±21.0

JNK2

95.3±1.0

PKA

109.2±15.3

PKCa

43.9±2.4

CLK2

78.5±5.5

TAK1

95.5±18.3

DDR2

109.4±7.8

HER4

46.2±15.1

MELK

79.5±14.7

STK33

96.3±7.0

MST2

109.6±30.2

DYRK1A

47.4±4.9

CSK

80.9±5.6

WNK1

97.0±1.4

OSR1

109.6±2.0

PKCÎł

50.1±8.0

GCK

81.2±11.9

CDK9

97.4±14.2

JAK2

109.7±8.0

PAK2

53.1±5.5

EPH-B3

81.8±2.8

ULK2

98.6±4.1

MINK1

112.6±15.4

ERK8

54.3±2.7

MSK1

82.7±6.8

PDGFRA

99.2±8.5

NEK6

113.0±24.7

EF2K

55.1±1.2

PINK

83.2±9.7

CK1δ

99.3±28.6

MEKK1

114.2±13.1

CHK2

56.2±1.9

MAP4K3

83.9±22.2

IRAK1

99.5±2.4

NEK2a

114.4±11.3

MKK2

57.0±6.9

IR

84.1±5.7

SRPK1

99.6±13.2

TGFBR1

116.0±26.8

NUAK1

58.5±11.6

SIK2

84.5±12.6

RSK1

99.7±5.0

MNK2

116.8±19.1

PIM1

59.5±13.7

PDK1

84.6±9.2

TTBK2

100.3±11.8

EPH-A2

118.8±15.6

SYK

61.3±5.8

SGK1

84.9±4.2

ASK1

100.5±17.0

SIK3

120.9±26.3

PAK5

62.3±6.9

MAPK-K2

86.6±9.9

ERK1

101.6±4.4

TESK1

121.0±11.0

FGF-R1

62.3±7.4

TAO1

87.0±1.7

ULK1

102.0±11.2

BTK

122.0±45.3

VEG-FR

65.4±4.3

LKB1

87.0±11.2

IGF-1R

102.4±3.9

MKK6

125.9±6.4

HIPK2

65.6±1.6

p38a MAPK

87.3±13.8

TTBK1

102.5±14.3

PAK6

127.3±2.3

CDK2

66.7±3.6

Src

87.4±14.8

TLK1

102.5±25.8

EPH-A4

127.5±5.0

DYRK2

67.5±5.0

MARK1

87.6±11.4

MST4

102.8±6.4

MPSK1

127.9±43.9

MARK4

70.5±1.5

RIPK2

88.1±22.1

BRK

103.0±24.0

IRR

131.0±37.3

IKKe

71.2±12.5

PIM2

88.3±3.9

ZAP70

104.0±8.2

p38g MAPK

131.3±22.8

DYRK3

71.6±2.7

MAP4K5

88.9±15.4

MST3

104.3±10.8

p38b MAPK

139.7±0.8

TTK

71.9±2.6

MLK1

89.1±3.6

RSK2

105.0±11.4

PKCz

145.1±17.1

JNK3

72.2±13.0

JNK1

89.8±7.8

CAMKKb

105.7±2.0

Lck

157.4±11.1

PRAK

72.8±0.1

PLK1

89.8±13.2

MARK2

105.8±0.2

EPH-B4

160.4±40.7

GSK3b

73.2±8.2

PKBb

90.0±11.3

MARK3

105.9±5.5

EPH-B1

190.1±4.6

S6K1

73.7±27.0

EIF2AK3

90.7±9.1

ABL

106.2±23.9

CHK1

190.6±4.0

EPH-B2

74.3±6.4

TBK1

91.2±12.5

HIPK1

106.4±27.1

  
  1. Results presented indicate the remaining activity of each kinase (average of two duplicate determinations ± standard deviation) in the presence of 500 nM of CuB. Inhibition of tropomyosin receptor kinase A (TrkA) by CuB is indicated in red font