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VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of Rheumatoid arthritis (RA). p38 MAPK is a specific enzyme that regulates the production of IL-1, IL-2, IL-6, TNFα, chemokines and nitric oxide (NO), as part of acute and chronic inflammatory responses. In vitro, VX-745 was selective for p38 MAPK compared to a large panel of kinases (IC50≥20µM). VX-745 selectively inhibited p38α MAPK (IC50=10 nM), p38β MAPK (IC50 =220 nM) [368149], but not p38γ MAPK (IC50≥20 µM). In addition, cell data for VX-745 provided IC50 values of 56 and 52 nM for IL-1β and TNFα, respectively, and VX-745 blocked IL-6 and IL-8 production induced by IL-1 and TNFα. In a human whole blood assay, IC50 values were 152 and 177 nM for IL-1β and TNFα inhibition, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | Human bone marrow stromal cells (BMSCs) and multiple myeloma (MM) cells |
| Preparation method | Incubating BMSCs (5 × 104 cells/well) or MM cells (3 × 104 cells/well) in 96-well culture plates in the presence or absence of VX-745 for 48 hours at 37 °C. Measuring DNA synthesis by [3H]-thymidine ([3H]TdR) uptake. Cells are pulsed with [3H]TdR (0.5 μCi/well [.0185 MBq]) during the last 8 hours of 48-hour cultures. Measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance to assess growth inhibition of both MM cells and BMSCs by VX-745 . |
| Concentrations | 60 nM - 20 μM, dissolved in DMSO. |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Type II collagen-induced arthritis (CIA) mice model (DBA/1J) |
| Formulation | Dissolved in 100% polyethylene glycol |
| Dosages | 2.5, 5, and 10 mg/kg |
| Administration | Oral gavage twice daily |
| Molecular Weight | 436.26 |
| Formula | C19H9Cl2F2N3OS |
| CAS Number | 209410-46-8 |
| Solubility (25°C) | DMSO 11 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] John P Duffy, et al. The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor
| Related p38 MAPK Products |
|---|
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| p38 MAP Kinase Inhibitor III
p38 MAP Kinase Inhibitor III is a p38 MAPK inhibitor with an IC50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with IC50 values of 0.37 μM and 0.044 μM, respectively. |
| (R)-STU104
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. |
| SB 706504
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| RWJ-67657
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. |
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