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Chemical Structure : GLPG3970
CAS No.: 2403733-82-2
Catalog No.: PC-20664Not For Human Use, Lab Use Only.
GLPG3970 (GLPG 3970) is a potent, selective first-in-class salt inducible kinase SIK2/SIK3 inhibitor with IC50 of 7.8/3.8 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $288 | In stock | |
| 10 mg | $458 | In stock | |
| 25 mg | $758 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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GLPG3970 (GLPG 3970) is a potent, selective first-in-class salt inducible kinase SIK2/SIK3 inhibitor with IC50 of 7.8/3.8 nM, respectively.
GLPG3970 exhibits high selectivity against a panel of 372 kinases, weakly inhibits SIK1 with IC50 of 282 nM.
GLPG3970 displays IC50 of >17,500 nM, 254 nM, and 79 nM on SIK1, SIK2, and SIK3, respectively in NanoBRET binding assays in HEK293 cells.
GLPG3970 inhibits the production of TNFα and IL-12, and increases the release of IL-10 by primary human myeloid cells and in human whole blood stimulated by LPS.
GLPG3970 (3, 10, or 30 mg/kg twice daily, po) shows concordant results on TNFα and IL-10 in vivo in mice challenged with LPS, displays significant efficacy in a mouse DSS colitis model.
| M.Wt | 504.51 | |
| Formula | C25H27F3N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
8-methoxy-6-(7-(2-morpholinoethoxy)imidazo[1,2-a]pyridin-3-yl)-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1(2H)-one |
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1. Peixoto C, et al. J Med Chem. 2024 Mar 29. doi: 10.1021/acs.jmedchem.3c02246.
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