118409-62-4

Usage

Biological Activity

ag-126 is an erk1 and erk2 inhibitor.extracellular signal-regulated kinases (erks) are widely expressed intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions. many different stimuli, such as growth factors, cytokines, transforming agents, and carcinogens, can activate the erk pathway.

in vitro

previous study found that r ag126 ould potently inhibit the pcw-evoked release and this effect was rather selective with respect to the stimulus. ag126 was found to be less potent in attenuating lps-triggered release. moreover, it was found that ag126 was able to prevent the pcw-inducible erk phosphorylation, which could relate to the ag126-mediated inhibition of pcw-evoked cytokine release [1].

in vivo

ag126 was tested in a model of pcw-induced meningitis, in which rats underwent intracisternal injection of pcw with and without ag126 pretreatment. pcw injection led to a dramatic leukocyte influx into the csf. ag126 treatment could significantly attenuate such invasion, without changing the number of circulating leukocytes. in addition, ag126 treatment showed beneficial effects on other parameters, such as intracranial pressure. furthermore, ag126 had no adverse effect on several physiological parameters including mean arterial blood pressure, arterial pao2, paco2 as well as ph [1].

IC 50

inhibits the phosphorylation of erk1 and erk2 at 25-50 μm

references

[1] hanisch, u. k.,prinz, m.,angstwurm, k., et al. the protein tyrosine kinase inhibitor ag126 prevents the massive microglial cytokine induction by pneumococcal cell walls. european journal of immunology 31, 2104-2115 (2001).

InChI:InChI=1/C10H5N3O3/c11-5-8(6-12)3-7-1-2-9(13(15)16)10(14)4-7/h1-4,14H

Upstream product

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Relevant academic research and scientific papers

Cosmetic composition

A composition suitable for topical application to mammalian skin and hair for inducing, maintaining or increasing hair growth comprises a hair growth promoter chosen from glutamine derivatives and salts thereof. The composition preferably also comprises an activity enhancer which may be chosen from hair growth stimulants, penetration enhancers and cationic polymers.

Cosmetic composition containing DOPA derivatives

A composition for topical application to human hair or skin contains a chemical analogue of dihydroxyphenyl alanine (DOPA). This chemical analogue can be absorbed by skin or by a hair follicle and metabolised in-vivo, thus leading to the formation of melanin in skin or to the growth of melanin-pigmented hair. Consequently the composition can give controlled skin darkening to mimic sun-induced tanning or can bring about the growth of dar hair in place of the grey or white hair.

Cosmestic composition

A composition suitable for topical application to mammalian skin and hair for inducing, maintaining or increasing hair growth comprises a hair growth promoter chosen from glutamic acid derivatives and salts thereof. The composition preferably also comprises an activity enhancer which may be chosen from hair growth stimulants, penetration enhancers and cationic polymers.

Tyrphostins I: Synthesis and Biological Activity of Protein Tyrosine Kinase Inhibitors

A novel class of low molecular weight proteine kinase inhibitors is described.These compounds consitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain.These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor.The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 102-103 higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases.These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors.The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth.These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases.We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.