1811510-56-1
1811510-56-1 structure
- Name: PF-06260933
- Chemical Name: PF06260933
- CAS Number: 1811510-56-1
- Molecular Formula: C16H13ClN4
- Molecular Weight: 296.75
- Catalog: Signaling Pathways MAPK/ERK Pathway MAP4K
- Create Date: 2018-01-29 10:31:03
- Modify Date: 2024-01-10 16:40:11
-
PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
| Name | PF06260933 |
|---|---|
| Synonyms |
5-(4-chlorophenyl)-3,3'-bipyridine-6,6'-diamine dihydrochloride
PF-06260933 |
| Description | PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively. |
|---|---|
| Related Catalog | |
| Target |
MAP4K4:3.7 nM (IC50) |
| In Vitro | PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro, similar to MAP4K4 knockdown[2]. |
| In Vivo | In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed[2]. |
| Cell Assay | HUVECs are maintained in EGM2 media at 37°C and 5% CO2. HUVECs or peritoneal macrophages are treated with vehicle or PF-06260933 in vitro to determine whether pharmacological inhibition of MAP4K4 alteres MAPK signalling in response to TNF-α[2]. |
| Animal Admin | Compound PF-06260933 (10 mg/kg, dissolved in dH2O) is orally administered to 8 to 10-week-old male Apoe-/- mice twice daily for 6 weeks. Ldlr-/- male mice are placed on high-fat diet (HFD) for 10 weeks before drug administration. Compound PF-06260933 is administered to male 8 to 10-week-old Ldlr-/- mice as above for 10 weeks. Oral administration of water is used as vehicle control in all studies. Mice are euthanized by CO2 inhalation followed by bilateral pneumothorax[2]. |
| References |
| Molecular Formula | C16H13ClN4 |
|---|---|
| Molecular Weight | 296.75 |
| Storage condition | 2-8℃ |