RWJ-67657

CHF 60.00
In stock
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Product Details
Synonyms RWJ67657
Product Type Chemical
Properties
Formula C27H24FN3O
MW 425.5
CAS 215303-72-3
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: p38 | Kinase Group: CMGC | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key QSUSKMBNZQHHPA-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
The cytokine Tumor necrosis factor-α (TNF-α) is secreted by activated monocytes/macrophages and T lymphocytes and has been implicated in several disease states, including rheumatoid arthritis, inflammatory bowel disease, septic shock, and osteoporosis. Monocyte/macrophage production of TNF-α is dependent on the mitogen-activated protein kinase p38. The compound RWJ 67657 is a potent, orally active inhibitor of MAPK and it inhibited the release of TNF-α from LPA stimulated human mononuclear cells with an IC(50) of 3nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the T cell stimulator and superantigen staphylococcal enterotoxin B with an IC(50) value of 13nM. Also RWJ 67657 was approximately 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all p38 dependent in vitro systems tested and is much more specific than SB 203580 for p38 kinaes. RWJ 67657 inhibited the enzymatic activity of recombinant p38α and β, with in vitro IC(50) values of 1 and 11µM respectively, but not γ or δ, and in further in vitro test across a panel of other enzymes RWJ 67657 demonstrated no other significant activity.
Product References
  1. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase: S.A. Wadsworth, et al.; J. Pharmacol. Exp. Ther. 291, 680 (1999)
  2. Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection: S. Wei, et al.; Antimicrob. Agents Chemother. 51, 4324 (2007)
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