| S0015 |
WNK-IN-11
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WNK-IN-11 is a potent, selective, and orally active allosteric inhibitor of With-No-Lysine (WNK) kinase with IC50 of 4 nM for WNK1 enzyme.
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| E1670 |
MKI-1
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MKI-1 (MASTL Kinase Inhibitor-1) is a small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in a kinase assay. It also exerts antitumor and radiosensitiser activities through PP2A-mediated c-Myc inhibition in breast cancer models.
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| E2396 |
STK16-IN-1
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STK16-IN-1 is a serine/threonine protein kinase 16 (STK16) inhibitor with an IC50 of 295 nM.
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| S3522 |
2OH-BNPP1
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2OH-BNPP1 is an inhibitor of the kinase activity of BUB1 (budding uninhibited by benzimidazoles-1, BUB1 Mitotic Checkpoint Serine/Threonine Kinase) that can be used for the treatment of cancer.
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| E0380 |
Hepln-13
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Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, which can be used for the research of metastatic prostate cancer.
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| S0995 |
BioE-1115
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BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively.
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| E2987 |
GCN2-IN-1
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GCN2-IN-1 (A-92) is a specific and potent active site inhibitor of general control nonderepressible 2 kinase (GCN2) with an IC50 of <0.3 μM. It can be investigated in research related to diseases involving retroviral integration.
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| S8864 |
ZT-12-037-01
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ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM.
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| E1120 |
TC-DAPK 6
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TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor with IC50 of 69 and 225 nM against DAPK1 and DAPK3, respectively.
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| S0848 |
GAK inhibitor 49
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GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with an IC50 of 56 nM.
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| S6060 |
HPK1-IN-2
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HPK1-IN-2 is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1, a serine/threonine Ste20-related protein kinase), Lck and Flt3 with IC50 of <0.05 μM, IC50 of <0.5 μM and IC50 of <0.05 μM, respectively. This compound exhibits antitumour activity.
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| E1975 |
HC-7366
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HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumour activity.
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| S8257 |
Luvixasertib (CFI-402257)
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Luvixasertib (CFI-402257) is an inhibitor of threonine tyrosine kinase (TTK) with an IC50 of 1.7 nM and Ki of 0.1 nM, respectively. It is a potential therapeutic for treating hepatocellular carcinoma that works directly by inhibiting cell-cycle checkpoints in cancer cells and indirectly by mobilising immune cells from the tumour microenvironment.
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| S6088 |
6-(Dimethylamino)purine
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6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits germinal vesicle breakdown and the meiotic maturation of oocytes.
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| E1065 |
SBP-3264
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SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukaemia (AML).
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| S7083 |
Ceritinib
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Ceritinib is a potent inhibitor against ALK with an IC50 of 0.2 nM in cell-free assays. This compound also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
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Signal Transduct Target Ther, 2025, 10(1):124
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Leukemia, 2025, 10.1038/s41375-025-02682-8
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Cell Mol Life Sci, 2025, 82(1):314
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| S4967 |
Ceritinib dihydrochloride
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Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitumour activity.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Exp Mol Med, 2022, 54(8):1225-1235
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Cancer Res, 2022, 82(2):307-319
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| E2836 |
ALK inhibitor 1
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ALK inhibitor 1 (compound 17) is a potent pyrimidine ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
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