SKF-86002

For research use only. Not for therapeutic Use.

  • CAT Number: I004712
  • CAS Number: 72873-74-6
  • Molecular Formula: C₁₆H₁₂F₃FS
  • Molecular Weight: 297.35
  • Purity: ≥95%
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<p style=/line-height:25px/>SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).<br>IC50 value:<br>Target: p38 MAPK inhibitor<br>in vitro: SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM) [1]. differentiation of HL-60 cells toward the neutrophil phenotype resulted in a loss in c-Jun NH2-terminal kinase activation with concomitant acquisition of formylmethionylleucylphenylalanine-stimulatable and stress-inducible p38 MAPK activity as well as apoptosis blockade by SKF-86002 [2]. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP [3].</p>


Catalog Number I004712
CAS Number 72873-74-6
Molecular Formula C₁₆H₁₂F₃FS
Purity ≥95%
Target p38 MAPK
Solubility 10 mM in DMSO
Storage Store at RT
InChI InChI=1S/C16H12FN3S/c17-13-3-1-11(2-4-13)14-15(12-5-7-18-8-6-12)20-9-10-21-16(20)19-14/h1-8H,9-10H2
InChIKey YOELZIQOLWZLQC-UHFFFAOYSA-N
SMILES C1CSC2=NC(=C(N21)C3=CC=NC=C3)C4=CC=C(C=C4)F
Reference

<p style=/line-height:25px/>
<br>[1]. Griswold DE, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70.
<br>[2]. Frasch SC, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97.
<br>[3]. Nick JA, et al. Common and distinct intracellular signaling pathways in human neutrophils utilized by platelet activating factor and FMLP. J Clin Invest. 1997 Mar 1;99(5):975-86.
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