RWJ 67657
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 1 and 11 μM for p38α and p38β, respectively
RWJ 67657 is an orally active inhibitor of the MAP kinases p38α and p38β.
Tumor necrosis factor-alpha (TNF-alpha), a cytokine secreted by activated monocytes/macrophages and T lymphocytes, is implicated in several disease states, such as inflammatory bowel disease, rheumatoid arthritis, septic shock, as well as osteoporosis. The monocyte/macrophage production of TNF-alpha is dependent on the mitogen-activated protein kinase p38.
In vitro: RWJ 67657 could inhibit the release of TNF-alpha by lipopolysaccharide-treated human peripheral blood mononuclear cells, as well as the release of TNF-alpha from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B. RWJ 67657 was about 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all tested p38 dependent in-vitro systems tested. Moreover, RWJ 67657 was able to inhibit the enzymatic activity of recombinant p38alpha and beta, but not gamma or delta, and showed no significant activity against various other enzymes. In contrast, SB 203580 could significantly inhibit the tyrosine kinases p56 lck and c-src. In addition, RWJ 67657 did not inhibit T cell production of interleukin-2 or interferon-gamma and did not inhibit T cell proliferation in response to mitogens [1].
In vivo: Animal study found that RWJ 67657 could inhibit TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Wadsworth, S. A.,Cavender, D.E.,Beers, S.A., et al. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. Journal of Pharmacology and Experimental Therapeutics 291(2), 680-687 (1999).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 425.5 |
Cas No. | 215303-72-3 |
Formula | C27H24FN3O |
Synonyms | JNJ-3026582 |
Solubility | ≤10mg/ml in ethanol;5mg/ml in DMSO;2mg/ml in dimethyl formamide |
Chemical Name | 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol |
SDF | Download SDF |
Canonical SMILES | FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)N(CCCC4=CC=CC=C4)C(C#CCCO)=N2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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