SKF 86002An inhibitor of p53, Cox, and 5-LO

SKF 86002 (CAS 72873-74-6)

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Synonym: 6-(4-fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo(2,1-b)thiazole
Application: An inhibitor of p53, Cox, and 5-LO
CAS Number: 72873-74-6
Molecular Weight: 297.4
Molecular Formula: C16H12FN3S
* Refer to Certificate of Analysis for lot specific data (including water content).
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SKF 86002 is a bicyclic imidazole that specifically inhibits p38 MAP kinase, and is also described as a cytokine-suppressant and an anti-inflammatory compound. SKF 86002 has been shown to inhibit Cox (cyclooxygenase) activity and 5-LO (5-lipoxygenase). Osteoblastic cell studies report that SKF 86002 inhibits the production of IL-6. SKF 86002 has been shown to block the activation of TNF-translation and potently inhibit IL-1.


References

1. Lee, J.C., et al. 1993. Ann. N.Y. Acad. Sci. 696: 149-170. PMID: 8109825
2. Prichett, W., et al. 1995. J. Inflamm. 45: 97-105. PMID: 7583362
3. Blanque, R., et al. 1997. Drugs Exp Clin Res. 23: 63-70. PMID: 9309381
4. Frasch, S.C., et al. 1998. J. Biol. Chem. 273: 8389-8397. PMID: 9525949
5. Yoo, B.K., et al. 2008. Neurochem. Int. 52: 1188-1197. PMID: 18289732
6. Santén, S., et al. 2009. Surgery. 145: 303-312. PMID: 19231583

Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/ml).
Storage :
Store at 4° C
Melting Point :
189-190° C (lit.)
Boiling Point :
476.11° C at 760 mmHg (Predicted)
Density :
1.39 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
p38α: IC50 = 0.11 µM (human); MAP kinase p38: IC50 = 0.4 µM (human); LPS-stimulated IL-1 and TNF-α production: IC50 = 1 µM; Cox-1: IC50 = 5.4 µM (human); 5-LO: IC50 = 10 µM (rat)
pK Values :
pKb: 4.36 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5228
MDL Number :
MFCD00869367
SMILES :
C1CSC2=NC(=C(N21)C3=CC=NC=C3)C4=CC=C(C=C4)F

Download SDS (MSDS)

Certificate of Analysis

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