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Chemical Structure : GLPG3312
Catalog No.: PC-21587Not For Human Use, Lab Use Only.
GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.
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GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.
GLPG3312 displays high selectivity against a panel of 380 kinases, RIPK2 is the most potent off-target with IC50 of 19.7 nM, which is 10-fold less potent than that on SIK1 and 30-fold less potent than those on SIK2 and SIK3.
GLPG3312 dose-dependently inhibits TNFα release in vitro cell assays using primary human monocytes and monocyte-derived macrophages (MdM) stimulated with LPS, with IC50 of 17 nM and 34 nM, respectively, also enhances the release of IL-10 at higher concentrations.
GLPG3312 displays both anti-inflammatory and immunoregulatory activities in vitro, inhibits the production of TNFα and increased the release of IL-10 in mice stimulated with LPS.
| M.Wt | 453.45 | |
| Formula | C23H21F2N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Temal-Laib T, et al. J Med Chem. 2023 Dec 26. doi: 10.1021/acs.jmedchem.3c01428.
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