Online Purchasing Account You are logged on as Guest. LoginRegister a New AccountShopping cart (Empty)
United States 

10Z-Hymenialdisine

MEK-1 inhibitor
 
ALX-350-289-M001 1 mg 380.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: BML-EI333

Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.MARK (microtubule affinity-regulating kinase) is potently inhibited by Hymenialdsine. In N2a cells stably transfected with htau40, Hymenialdisine (50µM) strongly inihibted neuritrite outgrowth.

Product Specification

Alternative Name:4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
 
Formula:C11H10BrN5O2
 
MW:324.1
 
Source:Isolated from sponge Axinella carteri.
 
CAS:82005-12-7
 
Purity:≥97% (HPLC)
 
Identity:Identity determined by 1H- NMR and MS.
 
Appearance:Yellow oil.
 
Solubility:Soluble in DMSO (5mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Handling:Protect from light.
 
350-289
Please mouse over
350-289

Product Literature References

Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004), Abstract;
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002), Abstract;
Protein kinase MARK/PAR-1 is required for neurite outgrowth and establishment of neuronal polarity: J. Biernat et al.; Mol. Biol. Cell. 13, 4013 (2002), Abstract;
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001), Abstract;
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001), Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000), Abstract;
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999), Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997), Abstract; Full Text
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997), Abstract; Full Text
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995), Abstract;
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982),

Related Literature

Brochures
Integrated solutions for screening Wnt regulators
Integrated solutions for screening Wnt regulators
Download as PDF

Catalogs
Diabetes Catalog
Diabetes Catalog
Download as PDF

Brochures
Essential Research Tools for Neurodegeneration & Neural Signaling
Essential Research Tools for Neurodegeneration & Neural Signaling
Download as PDF

Product Flyers
Cell Cycle - Mitosis, CDKS & Cell Cycle Signaling
Cell Cycle - Mitosis, CDKS & Cell Cycle Signaling
Download as PDF

Technical Posters
Disease-Associated Stress Signaling
Disease-Associated Stress Signaling
Download as PDF

All new literature pieces

Recommend this page

 
For Research Use Only. Not for use in diagnostic procedures.
Keep in touch

©2017 Enzo Life Sciences, Inc.,