420129

JNK Inhibitor V

The JNK Inhibitor V, also referenced under CAS 345987-15-7, controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: JNK Inhibitor V, SAPK Inhibitor V, 1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile, AS601245
• Fórmula empírica (notación de Hill): C₂₀H₁₆N₆S
• Número CAS: 345987-15-7
• Peso molecular: 372.45
• MDL number: MFCD07772196
• UNSPSC Code: 12352202
• NACRES: NA.77
• Assay: ≥95% (sum of two isomers, HPLC)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Propiedades

• Quality Segment: 100
• assay: ≥95% (sum of two isomers, HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated (hygroscopic), protect from light
• color: yellow
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: [s]1c2c(nc1C(c3nc(ncc3)NCCc4cnccc4)C#N)cccc2
• 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

Descripción

General description

A cell-permeable pyrimidinyl compound that displays anti-inflammatory properties. Acts as a potent, reversible, and ATP-competitive inhibitor of c-Jun N-terminal kinase (JNK, IC₅₀ = 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively) with a 10- to 100-fold greater selectivity over a panel of 25 other commonly studied kinases (IC₅₀ typically in the range of 1-10 µM or no effect at 10 µM). Its in vivo efficacy has been demonstrated in gerbils, mice, and rats via oral, i.v., or i.p. administration.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
hJNK 1, hJNK 2, hJNK 3

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Gaillard, P., et al. 2005. J. Med. Chem.48, 4596.
Carboni, S., et al. 2005. J. Neurochem.92, 1054.
Ferrandi, C., et al. 2004. Br. J. Pharmacol.142, 953.
Carboni, S., et al. 2004. J. Pharm. Exp. Ther.310, 25.

Soluble in DMSO, aliquot & store at -20*C; stable for 3 months

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Harmful (C)

Información de seguridad

• Clase de almacenamiento: 11 - Combustible Solids
• ¿Qué está pasando?: WGK 1