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SP600125

Chemical Structure : SP600125

CAS No.: 129-56-6

SP600125 (SP 600125;SP-600125)

Catalog No.: PC-42856Not For Human Use, Lab Use Only.

SP600125 is a potent, selective, reversible, ATP-competitive inhibitor of JNK with IC50 of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SP600125 (SP 600125) is a potent, selective, reversible, ATP-competitive inhibitor of JNK with IC50 of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.
SP600125 displays 300-fold selectivity against related MAP kinases ERK1 and p38, and PKA.
SP600125 dose dependently inhibits the phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-γ, TNF-α, and prevents the activation and differentiation of primary human CD4 cell cultures.
SP600125 blocks LPS-induced expression of TNF-α and inhibits anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes in vivo model of endotoxin-induced inflammation.
SP600125 also is a potent NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor, binds to the active pocket of NQO1 and inhibits NQO1 activity, inhibits NQO1-dependent cell death.

Physicochemical Properties

M.Wt 220.2261
Formula C14H8N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 45 mg/mL

Chemical Name/SMILES

Anthra[1,9-cd]pyrazol-6(2H)-one

References

1. Bennett BL, et al. Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13681-6.

2. Han Z, et al. J Clin Invest. 2001 Jul;108(1):73-81.

3. Gee K, et al. J Immunol. 2002 Nov 15;169(10):5660-72.

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