AS601245

AS601245

Catalog Number:
L002371333APE
Mfr. No.:
APE-B5942
Price:
$292
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      • Overview
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          Background

          Description:IC50: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectivelyRecent 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.

      • Properties
        • Alternative Name
          (Z)-2-(benzo[d]thiazol-2-yl)-2-(2-((2-(pyridin-3-yl)ethyl)imino)-1,2-dihydropyrimidin-4-yl)acetonitrile
          CAS Number
          345987-15-7
          Molecular Formula
          C20H16N6S
          Molecular Weight
          372.45
          Appearance
          A solid
          Purity
          98.50%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥14.25 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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