Home Metabolism Serine/threonin kinase

Serine/threonin kinase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8976 DCLK1-IN-1 DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. This compound inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
Clin Transl Med, 2022, 12(5):e743
S6710 SGC-GAK-1 SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase.
Cell Rep Med, 2025, S2666-3791(25)00231-9
Cell Reports Medicine, 2025, 102158
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.
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.
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.
Molecular Cancer Therapeutics, January 01 2018, 175-186
Oncotarget, December 29 2015, 44643-44659
ESMO Open, August 2021, 100172
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
bioRxiv, 2024, 2024.04.23.590638
Exp Mol Med, 2022, 54(8):1225-1235
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).