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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 CK1γ2 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
PKCγ 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