Serine/threonin kinase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S0015 WNK-IN-11 WNK-IN-11 is a potent, selective, and orally acitve allosteric inhibitor of With-No-Lysine (WNK) kinase with IC50 of 4 nM for WNK1 enzyme.
E1670 MKI-1 MKI-1(MASTL Kinase Inhibitor-1) is an small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in kinase assay. It also exerts antitumor and radiosensitizer activities through PP2A-mediated c-Myc inhibition in breast cancer models.
E2396 STK16-IN-1 STK16-IN-1 is a serine/threonine protein kinase 16 (STK16) inhibitor with an IC50 of 295 nM.
S3522 2OH-BNPP1 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.
E0380 Hepln-13 Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, can be used for the research of metastatic prostate cancer.
S0995 BioE-1115 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.
E2987 GCN2-IN-1 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.
S8864 ZT-12-037-01 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.
E1120 TC-DAPK 6 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.
S0848 GAK inhibitor 49 GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with an IC50 of 56 nM.
S6060 HPK1-IN-2 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 antitumor activity.
E1975 HC-7366 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-tumor activity.
S8257 Luvixasertib (CFI-402257) Luvixasertib (CFI-402257) is an inhibitor of threonine tyrosine kinase (TTK) with 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 mobilizing immune cells from the tumor microenvironment.
S6088 6-(Dimethylamino)purine 6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.
E1065 SBP-3264 SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).
S7083 Ceritinib (LDK378) Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
Signal Transduct Target Ther, 2025, 10(1):124
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Mol Life Sci, 2025, 82(1):314
Verified customer review of Ceritinib (LDK378)
S4967 Ceritinib dihydrochloride 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 antitomor activity.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).