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AS601245

Catalog No.
B5942
c-Jun NH2-terminal protein kinase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$138.00
In stock
1mg
$55.00
In stock
5mg
$132.00
In stock
10mg
$231.00
In stock
50mg
$891.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Description:

IC50: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively

Recent evidence suggests activation of the c-Jun NH2-terminal protein kinase (JNK) signal transduction pathway may play a role in ischemia-induced cell death. Therefore, preventing the activation of JNK, or c-Jun phosphorylation could be neuroprotective. AS601245 is a c-Jun NH2-terminal protein kinase inhibitor.

In vitro: AS601245 demonstrated a nonspecific inhibition of the three JNK human isoforms. AS601245 inhibits isolated hJNK3 in an ATPcompetitive manner. Selectivity of AS601245 was tested against a large panel of kinases. It exhibited 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Tyr- and Ser/Thr-protein kinases [1].

In vivo: AS601245 administered i.p. provided significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia. This effect is mediated by JNK inhibition and thus by c-Jun expression and phosphorylation. A significant neuroprotective effect of AS601245 administered either by i.p. injection or as i.v. bolus followed by an i.v. infusion was also observed in rats after focal cerebral ischemia [1].

Clinical trial: Up to now, AS601245 is still in the preclinical development stage.

Reference:
[1] Carboni S, Hiver A, Szyndralewiez C, Gaillard P, Gotteland JP, Vitte PA.  AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. J Pharmacol Exp Ther. 2004 Jul;310(1):25-32. Epub 2004 Feb 26.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt372.45
Cas No.345987-15-7
FormulaC20H16N6S
Solubilityinsoluble in H2O; insoluble in EtOH; ≥14.25 mg/mL in DMSO
Chemical Name(Z)-2-(benzo[d]thiazol-2-yl)-2-(2-((2-(pyridin-3-yl)ethyl)imino)-1,2-dihydropyrimidin-4-yl)acetonitrile
SDFDownload SDF
Canonical SMILESN#CC(C1=NC2=CC=CC=C2S1)C(C=CN/3)=NC3=N/CCC4=CN=CC=C4
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

AS601245