| S7565 |
WH-4-023
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WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
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Stem Cell Res Ther, 2025, 16(1):527
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Stem Cell Res Ther, 2025, 16(1):617
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Commun Biol, 2025, 8(1):125
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| S8393 |
HG-9-91-01
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HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective inhibitor of salt-inducible kinase (SIK) with IC50 of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3, respectively.
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J Biol Chem, 2025, 301(8):110434
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Nature Metabolism, 2024, 1310-1328
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Elife, 2024, 13RP96852
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| S8543 |
ARN-3236
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ARN-3236 is a potent, orally available and selective inhibitor of salt-inducible kinase 2 (SIK2) with IC50 of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. This compound induces apoptosis in cancer cells.
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J Biol Chem, 2025, 301(8):110434
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Int J Biol Sci, 2024, 20(1):312-330
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Mol Oncol, 2022, 16(13):2558-2574
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| S9646 |
YKL-05-099
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YKL-05-099 is an inhibitor of salt-inducible kinase (SIK) with IC50 of ~10 nM, ~40 nM and ~30 nM for SIK1, SIK2 and SIK3, respectively.
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Oncogenesis, 2022, 18
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Oncogenesis, 2022, 11(1):18
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Int J Hematol, 2020, 10.1007/s12185-020-03026-1
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| E5798New |
GLPG3312
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GLPG3312 is a potent and selective inhibitor of pan-SIK, with an IC50 of 2.0 nM for SIK1, 0.7 nM for SIK2, and 0.6 nM for SIK3. It demonstrates anti-inflammatory and immunoregulatory activities in vitro in human primary myeloid cells and in vivo in mouse models.
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| S0051 |
YKL 06-061
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YKL 06-061 is a potent and selective salt-inducible kinase (SIK) inhibitor with IC50 of 6.56 nM, 1.77 nM and 20.5 nM for SIK1, SIK2 and SIK3, respectively.
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| E1997 |
GLPG3970
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GLPG3970 (compound 32) is a dual inhibitor of SIK2 and SIK3, with IC50 of 282.8 nM, 7.8 nM and 3.8 nM for SIK1, SIK2 and SIK3, respectively. It has the potential to treat autoimmune and inflammatory diseases.
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