| AS601245c-Jun NH2-terminal protein kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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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.
