| Name | GLPG0634 analog |
| Description | GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively. |
| Kinase Assay | EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1]. |
| In vitro | In multiple cell lines, GLPG0634 inhibited IFN-αB2-induced JAK1/TYK2 type II receptor signaling and IL-2/4-induced JAK1/JAK3/γc signaling (IC50: 150-760 nM). At the cellular level, GLPG0634 was more selective for JAK1-containing JAK/STAT signaling than JAK2 kinase. In addition, GLPG0634 inhibited the proliferation of Th1/Th2/Th17 cells. |
| In vivo | In multiple cell lines, GLPG0634 inhibited IFN-αB2-induced JAK1/TYK2 type II receptor signaling and IL-2/4-induced JAK1/JAK3/γc signaling (IC50: 150-760 nM). At the cellular level, GLPG0634 was more selective for JAK1-containing JAK/STAT signaling than JAK2 kinase. In addition, GLPG0634 inhibited the proliferation of Th1/Th2/Th17 cells. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 7.5 mg/mL (18.27 mM), Sonication is recommended.
|
| Keywords | TyrosineKinases | Tyrosine Kinases | TYK2 | OSM/IL-lβ | Janus kinase | JAK3 | JAK2 | JAK1 | JAK | Inhibitor | inhibit | Hela cell | GLPG-0634 analog | GLPG0634 analog | GLPG-0634 | GLPG0634 | GLPG 0634 | AK-STAT |
| Inhibitors Related | Delgocitinib | Deucravacitinib | RO8191 | Tofacitinib Citrate | GSK 3 Inhibitor IX | CEP-33779 | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Fedratinib | Tofacitinib | Gefitinib |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library |
United States
