A potent JNK inhibitor used in cells and animals
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JNK Inhibitor V

Item No. 17542

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
a-[2-[[2-(3-pyridinyl)ethyl]amino]-4-pyrimidinyl]-2-benzothiazoleacetonitrile
CAS Number
345987-15-7
Synonyms
  • AS-601245
  • c-Jun N-terminal Kinase Inhibitor V
Molecular Formula
C20H16N6S
Formula Weight
372.5
Purity
≥98% (sum of isomers)
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/ml
SMILES
N#CC(C1=NC(NCCC2=CC=CN=C2)=NC=C1)C3=NC4=CC=CC=C4S3
InChi Code
InChI=1S/C20H16N6S/c21-12-15(19-25-17-5-1-2-6-18(17)27-19)16-8-11-24-20(26-16)23-10-7-14-4-3-9-22-13-14/h1-6,8-9,11,13,15H,7,10H2,(H,23,24,26)
InChi Key
RCYPVQCPYKNSTG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $62

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    5 mg

    $164

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    10 mg

    $295

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    25 mg

    $589

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    Product Description

    c-Jun N-terminal kinases (JNKs) phosphorylate c-Jun and regulate transcription in response to an array of inflammatory signals.1 JNK inhibitor V is an ATP-competitive inhibitor of JNK1, JNK2, and JNK3 (IC50s = 150, 220, and 70 nM, respectively).2,3 While initial studies demonstrated 10- to 100-fold selectivity for JNK isoforms over a panel of 25 other kinases, strong interactions of JNK inhibitor V with GSK3B, Pim-1, Pim-3, and other kinases, evaluated as a shift in thermal melting point, suggest additional targets exist.2,4 In vivo efficacy of JNK inhibitor V against JNK isoforms has been demonstrated in gerbils, mice, and rats via oral, intravenous, or intraperitoneal administration.4,5 This compound is commonly used to investigate the role of JNK signaling in cells and animals.6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johnson, G.L., and Lapadat, R. Mitogen-activated protein kinase pathways mediated by ERK, JNK, and p38 protein kinases. Science 298(5600), 1911-1912 (2002).

    2. Gaillard, P., Jeanclaude-Etter, I., Ardissone, V., et al. Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. J. Med. Chem. 48(14), 4596-4607 (2005).

    3. Carboni, S., Hiver, A., Szyndralewiez, C., et al. 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. 310(1), 25-32 (2004).

    4. Fedorov, O., Marsden, B., Pogacic, V., et al. A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc. Natl. Acad. Sci. USA 104(51), 20523-20528 (2007).

    5. Ferrandi, C., Ballerio, R., Gaillard, P., et al. Inhibition of c-Jun N-terminal kinase decreases cardiomyocyte apoptosis and infarct size after myocardial ischemia and reperfusion in anaesthetized rats. Br. J. Pharmacol. 142(6), 953-960 (2004).

    6. Oktem, O., Buyuk, E., and Oktay, K. Preantral follicle growth is regulated by c-Jun-N-terminal kinase (JNK) pathway. Reprod.Sci. 18(3), 269-276 (2011).

    7. Tu, Y.F., Tsai, Y.S., Wang, L.W., et al. Overweight worsens apoptosis, neuroinflammation and blood-brain barrier damage after hypoxic ischemia in neonatal brain through JNK hyperactivation. J. Neuroinflammation 8:40, (2011).