All AbMole products are for research use only, cannot be used for human consumption.
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 |
|---|
| BIRB796
BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Selonsertib
GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. |
| Adezmapimod
Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. |
| SB 202190
SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase with IC50 values of 50 and 100 nM inhibiting p38α and p38β, respectively. |
| PH-797804
PH-797804 is a highly selective and potent inhibitor of p38 MAP kinase with IC50 of 26 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
