| AS601245c-Jun NH2-terminal protein kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.74%
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| Cas No. | 345987-15-7 | SDF | Download SDF |
| Chemical Name | (Z)-2-(benzo[d]thiazol-2-yl)-2-(2-((2-(pyridin-3-yl)ethyl)imino)-1,2-dihydropyrimidin-4-yl)acetonitrile | ||
| Canonical SMILES | N#CC(C1=NC2=CC=CC=C2S1)C(C=CN/3)=NC3=N/CCC4=CN=CC=C4 | ||
| Formula | C20H16N6S | M.Wt | 372.45 |
| Solubility | ≥14.25mg/mL in DMSO, ≥10mg/mL in H2O with gentle warming | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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