TYRPHOSTIN AG 126 Property

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

≤0.15mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide

form 

Yellow solid

color 

Light yellow to yellow

Sensitive 

Light Sensitive

Safety

Hazard Codes 

T

Risk Statements 

23/24/25

Safety Statements 

26-36-45

WGK Germany 

3

HazardClass 

6.1

HS Code 

2926907090

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

TYRPHOSTIN AG 126 Chemical Properties,Usage,Production

Definition

ChEBI: 2-[(3-hydroxy-4-nitrophenyl)methylidene]propanedinitrile is a nitrophenol.

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).