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Merck - 506174-5MG - p38 MAP Kinase Inhibitor XIX, Skepinone-L - Calbiochem

  • MFR SKU: 506174-5MG
  • ITEM #: 13025578
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ITEM #: 13025578
p38 MAP Kinase Inhibitor XIX, Skepinone-L
, 5MG
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Merck - 506174-5MG - p38 MAP Kinase Inhibitor XIX, Skepinone-L - Calbiochem

  • Item #: 13025578
  • MFR SKU: 506174-5MG
  • Overview A cell-permeable phenylamino-dibenzosuberone-diol with a rigid molecular structure specifically designed to target hydrophobic region I in p38α & p38β, but not in other kinases with bulky entrance-blocking gatekeeper residues. Shown to selectively inhibit p38α (IC 50 = 5 nM; [ATP] = 100 µ M) and p38β (97% inhibition at1 µ M), while exhibiting little affinity toward 400 other kinase constructs, including p38δ, p38γ, Erk1/2/3/4/5/8, JNK1/2/3, and MEK1/2/3/4/6. Shown to prevent cellular HSP27 Ser82 phosphorylation upon p38 activation by Anisomycin (Cat. No. 176880 ) in HeLa (IC 50 = 25 nM) or by TNF-α in THP-1 cultures. Unlike the ATP-binding site-targeting BIRB 796 (Cat. No. 506172 ) and SB 203580 (Cat. Nos. 559389 , 559395 , and 559398 ), Skepinone-L does not inhibit JNK-mediated c-Jun or ERK-dependent CREB phosphorylation in THP-1 cultures. Oral administration to D-Gal- (Cat. No. 34539 ) sensitized mice is reported to greatly reduce plasma TNF-α production upon LPS (Cat. No. 437625 ) challenge (by 77%; 3 mg/kg p.o.) in vivo .
  • Catalogue Number 506174
  • Brand Family Calbiochem®
  • Synonyms (2-(2, 4-Difluorophenylamino)-7-[2 R -, 3-dihydroxypropoxy]-10, 11-dihydro-dibenzo[a, d]-cyclohepten-5-one)
  • References Koeberle, S.C., et al. 2012. J. Med. Chem. 55, 5868.
  • Koeberle, S.C., et al. 2011. Nat. Chem. Biol. 8, 141.
  • Form Light yellow powder
  • Hill Formula CHFNO
  • Chemical formula CHFNO
  • Structure formula Image
  • Quality Level MQ100
  • Purity ≥ 99% by HPLC
  • Ship Code Ambient Temperature Only
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 6 months at -20° C.
  • Packaged under inert gas Packaged under inert gas

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