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LL-Z1640-2

Protein kinase inhibitor
 
ALX-380-267-M001 1 mg 56.00 USD
 
ALX-380-267-M005 5 mg 240.00 USD
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Inhibitor of the JNK/p38 pathways. Inhibits anisomycin-induced but not TNF-induced JNK/p38 activation. Potent protein kinase inhibitor.
A naturally isolated cell-permeable fungal resorcylic lactone that acts as a selective and highly potent inhibitor against the MAPKKK TAK1 activity (IC50 = 8nM) in an ATP-competitive and irreversible manner; also inhibits MEK1 (IC50 = 411nM) and three other MAPKKKs (IC50 ≥268 nM against MEKK1, ASK1, and MEKK4) but at much higher concentrations. Shown to inhibit IL-1-induced/TAK1-mediated, but not H2O2-induced/TAK1-independent, JNK and p38 phosphorylation in 293 cells.

Product Specification

Alternative Name:(5Z)-7-Oxozeaenol
 
Formula:C19H22O7
 
MW:362.4
 
Source:Isolated from Deuteromycetes sp.
 
CAS:253863-19-7
 
Purity:≥95% (HPLC)
 
Appearance:White to off-white solid.
 
Solubility:Soluble in methanol, acetone, DMSO (up to 25mM) or ethyl acetate; insoluble in ethanol and n-hexane.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
380-267
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380-267

Product Literature References

TAK1 inhibition promotes apoptosis in KRAS-dependent colon cancers: A. Singh, et al.; Cell 148, 639 (2012), Abstract;
In vivo RNAi-mediated silencing of TAK1 decreases inflammatory Th1 and Th17 cells through targeting of myeloid cells: G. Courties, et al.; Blood 116, 3505 (2010), Abstract;
Targeting innate immunity protein kinase signalling in inflammation: M. Gaestel, et al.; Nat, Rev. Drug Discov. 8, 480 (2009), Abstract;
Chemistry and biology of resorcylic acid lactones: N. Winssinger & S. Barluenga; Chem. Commun. 1, 22 (2007), (Review), Abstract; Full Text
Molecular mechanisms involved in the regulation of cytokine production by muramyl dipeptide: M. Windheim, et al.; Biochem. J. 404, 179 (2007), Abstract;
Protein kinases as small molecule inhibitor targets in inflammation: M. Gaestel, et al.; Curr. Med. Chem. 14, 2214 (2007), (Review), Abstract;
Blockade of transforming growth factor-beta-activated kinase 1 activity enhances TRAIL-induced apoptosis through activation of a caspase cascade: M.K. Choo, et al.; Mol. Cancer Ther. 5, 2970 (2006), Abstract;
Involvement of the extracellular signal-regulated protein kinase pathway in phosphorylation of p53 protein and exerting cytotoxicity in human neuroblastoma cells (SH-SY5Y) exposed to acrylamide: T. Okuno, et al.; Arch. Toxicol. 80, 146 (2006), Abstract;
JNK (c-Jun NH2 terminal kinase) and p38 during ischemia reperfusion injury in the small intestine: T. Murayama, et al.; Transplantation 81, 1325 (2006), Abstract;
Transforming growth factor beta-activated kinase 1 is a key mediator of ovine follicle-stimulating hormone beta-subunit expression: N. Safwat, et al.; Endocrinology 14, 4814 (2005), Abstract;
Suppression of cadmium-induced JNK/p38 activation and HSP70 family gene expression by LL-Z1640-2 in NIH3T3 cells: N. Sugisawa, et al.; Toxicol. Appl. Pharmacol. 196, 206 (2004), Abstract;
A resorcylic acid lactone, 5Z-7-oxozeaenol, prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase: J. Ninomiya-Tsuji, et al.; J. Biol. Chem. 278, 18485 (2003), Abstract;
Effects of pentachlorophenol and tetrachlorohydroquinone on mitogen-activated protein kinase pathways in Jurkat T cells: B. Wispriyono, et al.; Environ. Health Perspect. 110, 139 (2002), Abstract; Full Text
Pharmacological inhibitors of MAPK pathways: J.M. English & M.H. Cobb; TIPS 23, 40 (2002), (Review), Abstract;
Cadmium induces phosphorylation of p53 at serine 15 in MCF-7 cells: M. Matsuoka & H. Igisu; BBRC 282, 1120 (2001), Abstract;
Inhibition of HgCl2-induced mitogen-activated protein kinase activation by LL-Z1640-2 in CCRF-CEM cells: M. Matsuoka, et al.; Eur. J. Pharmacol. 409, 155 (2000), Abstract;
A radicicol-related macrocyclic nonaketide compound, antibiotic LL-Z1640-2, inhibits the JNK/p38 pathways in signal-specific manner: K. Takehana, et al.; BBRC 257, 19 (1999), Abstract;

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