GLPG3970 | SIK2/SIK3 inhibitor | Probechem Biochemicals

Chemical Structure : GLPG3970

CAS No.: 2403733-82-2

GLPG3970 (GLPG 3970, GLPG-3970)

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
5 mg	$288	In stock
10 mg	$458	In stock
25 mg	$758	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	504.51
Formula	C25H27F3N4O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
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

References

1. Peixoto C, et al. J Med Chem. 2024 Mar 29. doi: 10.1021/acs.jmedchem.3c02246.

GLPG3970 (GLPG 3970, GLPG-3970)

Biological Activity

Physicochemical Properties

References

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