Shopping Cart
Remove All
Your shopping cart is currently empty
GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis. |
| Targets&IC50 | SIK2:0.3 nM |
| In vitro | GLPG4970 (Compound 8) inhibits various off-target kinases, with IC₅₀ values ranging from 4 nM to 292 nM. It induces nuclear translocation of CRTC3 in U2OS cells, with an EC₅₀ of 16 nM. In lipopolysaccharide-stimulated monocytes and macrophages, GLPG4970 dose-dependently inhibits TNFα release, with IC₅₀ values of 3.6 nM and 8.1 nM, respectively, and enhances IL-10 release. |
| In vivo | GLPG4970 (Compound 8) administered orally at doses of 0.5-30 mg/kg 15 minutes before LPS exposure reduces TNFα release and enhances IL-10 release in LPS-treated mice. Additionally, GLPG4970 at doses of 3-30 mg/kg, given orally twice daily, slows the progression of disease in a mouse model of colitis induced by dextran sulfate sodium (DSS). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Size | Quantity | Unit Price | Amount | Operation |
|---|

Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.