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Neflamapimod

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Catalog No. T6089Cas No. 209410-46-8
Alias VX-745

Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.

Neflamapimod

Neflamapimod

🥰Excellent
Purity: 99.75%
Catalog No. T6089Alias VX-745Cas No. 209410-46-8
Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.
Pack SizePriceAvailabilityQuantity
5 mg40 €In Stock
10 mg66 €In Stock
25 mg121 €In Stock
50 mg206 €In Stock
100 mg306 €In Stock
200 mg457 €In Stock
1 mL x 10 mM (in DMSO)44 €In Stock
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Purity:99.75%
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Product Introduction

Bioactivity
Description
Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.
Targets&IC50
p38α:10 nM, p38β:220 nM
In vitro
Neflamapimod selectively inhibits p38α and p38β MAPK with IC50 of 10 nM and 220 nM, respectively, but not p38γ MAPK and a large panel of other kinases, with IC50 larger than 20 μM. In a human peripheral blood mononuclear cell (PBMC) assay, Neflamapimod provides IC50 of 56 and 52 nM for IL-1β and TNFα, respectively. Neflamapimod blocks IL-6 and IL-8 production induced by IL-1 and TNFα, and COX-2 synthesis mediated by LPS and IL-1β. [1-3] Neflamapimod (60 nM-20 μM) inhibits IL-6 and VEGF secretion in bone marrow stromal cells (BMSCs), without affecting their viability. Neflamapimod also inhibits TNF-α-induced IL-6 secretion in BMSCs. Neflamapimod inhibits both multiple myeloma (MM) cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs, suggesting that Neflamapimod can inhibit paracrine multiple myeloma (MM) cell growth in the BM milieu and overcome cell adhesion-related drug resistance. [4]
In vivo
Neflamapimod is effective against adjuvant-induced arthritis (AA) in the rat with ED50 of 5 mg/kg. Histological scores for Neflamapimod in AA rats are 93% inhibition of bone resorption and 56% inhibition of inflammation. In the classical cartilage-induced arthritis model, Neflamapimod exhibits a dose-responsive decrease in severity score. [1-3] In a type II collagen-induced arthritis (CIA) mice model, Neflamapimod (2.5, 5, and 10 mg/kg) has 27%, 31%, and 44% improvement in the inflammatory scores, respectively, when compared to vehicle-treated mice. In addition, histological scores show a 32-39% protection of bone and cartilage erosion by Neflamapimod. [5]
Kinase Assay
Spectrophotometric coupled-enzyme assay: The IC50 for the inhibition of p38α and p38β homologs are obtained by a spectrophotometric coupled-enzyme assay. A fixed concentration of enzyme (15 nM of p38α or p38β) is incubated with VX-745 in DMSO for 10 min. at 30 °C in 0.1 M HEPES buffer, pH 7.5, containing 10% glycerol, 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase, and 200 μM EGF receptor peptide (KRELVEPLTPSGEAPNQALLR). The reaction is initiated with 100 μM and 70 μM ATP for p38α and p38β assays, respectively. The decrease of absorbance at 340 nm is monitored to follow the rate of the reaction. IC50 is evaluated from the rate data as a function of the inhibitor concentration.
Cell Research
BMSCs (5 × 104 cells/well) or MM cells (3 × 104 cells/well) are incubated in 96-well culture plates in the presence or absence of VX-745 for 48 hours at 37 °C. DNA synthesis is measured 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. Growth inhibition of both MM cells and BMSCs by VX-745 is also assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance.(Only for Reference)
AliasVX-745
Chemical Properties
Molecular Weight436.26
FormulaC19H9Cl2F2N3OS
Cas No.209410-46-8
SmilesFc1ccc(Sc2ccc3c(-c4c(Cl)cccc4Cl)c(=O)ncn3n2)c(F)c1
Relative Density.1.55g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 43.6 mg/mL (100 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2922 mL11.4611 mL22.9221 mL114.6106 mL
5 mM0.4584 mL2.2922 mL4.5844 mL22.9221 mL
10 mM0.2292 mL1.1461 mL2.2922 mL11.4611 mL
20 mM0.1146 mL0.5731 mL1.1461 mL5.7305 mL
50 mM0.0458 mL0.2292 mL0.4584 mL2.2922 mL
100 mM0.0229 mL0.1146 mL0.2292 mL1.1461 mL

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