1,9-Pyrazoloanthrone_small.pngSP600125 is a JNK-1,-2,-3 Kinase Inhibitor:

(Product No. S-2022, AG Scientific, Inc.)

Purity: >98% (HPLC)

Synonym: 1,9-Pyrazoloanthrone, Anthrapyrazolone

Empirical Formula: C14H8N2O

Molecular Weight: 220.23 g/mol

CAS Number: 129-56-6

MDL number: MFCD00022289

PubChem Substance ID: 24278395

Some features and benefits include:

  1. SP600125 is a new and potent selective inhibitor of JNK-1,-2, and -3 (Ki = 0.19 µM). When activated, SP600125 offers researchers an improved selectivity (>20 fold) to inhibition when compared to a range of other kinases and enzymes.
  2. Inhibits phosphorylation of c-Jun, thus blocking the expression of inflammatory response genes IL-2, COX-2, TNF-α, IFN-γ. Blocks the activation and differentiation of primary human CD4 immune cells in culture.
  3. SP600125 inhibits TNF-α mRNA expression preventing bacterial sepsis including the apoptosis of anti-T cell pre-cursors CD4+ CD8+ thymocytes, in other animal studies [1].

SP600125 also inhibits the initiation of c-Jun transcriptional mRNA in synoviocytes required for good joint health. [Han, Z., et al. "c-Jun N-terminal kinase is required for metalloproteinase expression and joint destruction in inflammatory arthritis." J. Clin. Invest. 108: 73-81 (2001).]

Here are some of the reasons why SP600125 is an effective JNK Inhibitor:

  • Reduces the levels of c-Jun phosphorylation
  • Prevents apoptosis in dopaminergic neurons
  • Partially reverses the loss of dopamine in MPTP-induced Parkinson's disease in mice.

*Wang W., et al.  "SP600125, a new JNK inhibitor, protects dopaminergic neurons in the MPTP model of Parkinson's disease." Neurosci. Res. 48: 195-202 (2004).


JNK Kinase Inhibitors:

The stress-activated protein kinase, c-Jun-amino-terminal kinase (SAPK/JNK) is potently and preferentially activated by a variety of environmental stresses including UV and gamma radiation, ceramides, inflammatory cytokines, and in some instances, growth factors and GPCR agonists.

Here is a list of related A.G. Scientific, Inc. products:

SB-20358

SB-203580 is a pyridinyl imidazole which acts as a specific inhibitor of p38 MAP Kinase. SB-203580 does not inhibit the MAP kinase homologs JNK and p42 MAP kinase.

DASATINIB

Dasatanib is a multi-kinase inhibitor with potent activity against Bcr-Abl kinase (IC50 = 0.2-1.1 nM). Dasatinib also inhibits Lyn (IC50 = 8.5 nM) and Src (IC50 = 3.0 nM) kinase activities in vitro using 0.1 mg/mL poly (Glu4-Tyr) as the substrate. Dasatinib is used to treat certain adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (CML) or acute lymphoblastic leukemia (ALL).

LAPATINIB DITOSYLATE

Lapatinib is a potent inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM), ErbB-4 kinase (Ki = 347 nM). Lapatinib can restore tamoxifen sensitivity in tamoxifen-resistant, ER-positive breast cancer models.

DISCOVERYPAK EGFR TYROSINE KINASE INHIBITOR SET

A convenient set consisting of five Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase (TK) inhibitors. The five inhibitors are: 5 mg of Canertinib (Cat. No. 1617-5), 100 mg of Erlotinib, Hydrochloride (Cat. No. 1588-100), 5 mg of Gefitinib (Cat. No. 1589-5), 25 mg of Lapatinib, Ditosylate (Cat. No. 1624-25), and 2 mg of PD 153035 Hydrochloride (Cat. No. 1656-2).

DISCOVERYPAK RECEPTOR TYROSINE KINASE (RTK) INHIBITOR SET

A convenient set consisting of eight Receptor Tyrosine Kinase (RTK) inhibitors. The eight inhibitors are: 5 mg of Axitinib (Cat. No. 1581-5), 5 mg of Canertinib (Cat. No. 1617-5), 5 mg of Gefitinib (Cat. No. 1589-5), 5 mg of GW2580 (Cat. No. 1740-5), 25 mg of Lapatinib Ditosylate (Cat. No. 1624-25), 1 mg of PD-173074 (Cat. No. 1675-1), 1 mg of SB-431542 (Cat. No. 1674-1), and 100 mg of Sunitinib Malate (Cat. No. 1611-100).

PATHWAYREADY EGFR SIGNALING INHIBITOR PANEL

A convenient set consisting of fourteen inhibitors useful for the study of EGFR signaling pathway. The fouteen inhibitors are: 5 mg of AG 490 (Cat. No. 1570-5), 1 mg of Akt Inhibitor, Isozyme-Selective (Cat. No. 1708-1), 5 mg of Canertinib (Cat. No. 1617-5), 5 mg of Gefitinib (Cat. No. 1589-5), 25 mg of Lapatinib Ditosylate (Cat. No. 1624-25), 5 mg of LY 294002 (Cat. No. 1667-5), 5 mg of PD 98059 (Cat. No. 1666-5), 1 mg of PP2 (Cat. No. 1767-1), 1 mg of Rapamycin (Cat. No. 1568-1), 1 mg of SB 203580 (Cat. No. 1712-1), 25 mg of Sorafenib (Cat. No. 1594-25), 5 mg of SP 600125 (Cat. No. 1669-5), 5 mg of Stat3 Inhibitor, S3I-201 (Cat. No. 1775-5), and 1 mg of ZM 336372 (Cat. No. 1789-1)


AG Scientific: A leader in protein kinases:

Protein kinases are a family of kinases that functionally change specific proteins via phosphorylation. Protein kinases are involved in the regulation of signal transduction and many other cellular pathways. Many researchers have had success with Calmodulins & Geldanamycin.

For more information, go to: http://www.agscientific.com/inhibitors.html

 

[1] Bennett, B.L., et al. "SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase." Proc. Natl. Acad. Sci. USA 98: 13681-13686 (2001).

 

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  1. SP600125 chemical structure | CAS 129-56-6 | Cell-permeable reversible inhibitor of JNK | AG Scientific, Inc.
    SP600125
    S-2022

    Starting at $64.99

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