| Name | GSK805 |
| Description | GSK805 is a potent, orally bioavailable and CNS-penetrant RORγt inhibitor. |
| Cell Research | CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1]. |
| In vitro | METHODS: CD4 T cells (activated under Th17 cell differentiation conditions) were treated with GSK805 (0.5 μM, 4 days). IL-17 and IFNγ production was measured by intracellular cytokine staining.
RESULTS GSK805 exerted an inhibitory effect on Th17 cell differentiation. [1] |
| In vivo | METHODS: C57BL/6 mice were induced to develop EAE and treated with GSK805 (30 mg/kg, p.o., 14 days). CNS-infiltrating cells were isolated, and IL-17 and IFNγ production was measured by intracellular staining.
RESULTS GSK805 strongly inhibited Th17 cell responses in the CNS (reduced IFNγIL-17 and IFNγIL-17 T cells), whereas the frequency of TNF-α T cells was not significantly altered). [1]
METHODS: GSK805 (1, 3 and 10 mg/kg, orally, three times a day) was administered to EAE mice to observe its effects on the mice.
RESULTS GSK805 can reduce the clinical severity of EAE in a dose-dependent manner. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (18.78 mM), Suspension.
DMSO : 100 mg/mL (187.84 mM), Sonication is recommended.
|
| Keywords | Th17 cell | RORγt | ROR | RAR-related orphan receptor | oral | Inhibitor | inhibit | immunity | GSK-805 | GSK805 | GSK 805 | CNS penetrant |
| Inhibitors Related | S18-000003 | T0901317 | GSK2981278 | MRL-871 | Nobiletin | XY101 | AZD-0284 | Melatonin | SR2211 | SR 1903 | Cholesterol | ML 209 |
| Related Compound Libraries | Nuclear Receptor Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Metabolism Compound Library | Orally Active Compound Library | Lipid Metabolism Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Transcription Factor-Targeted Compound Library |
United States
