420150-M

JNK Inhibitor XVI, JNK-IN-8

The JNK Inhibitor XVI, JNK-IN-8 controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): JNK Inhibitor XVI, JNK-IN-8, (E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
• Fórmula empírica (Notação de Hill): C₂₉H₂₉N₇O₂
• Número CAS: 1410880-22-6
• Peso molecular: 507.59
• Número MDL: MFCD22124890
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥97% (HPLC)
• forma: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light yellow to yellow
• solubilidade: DMSO: 100 mg/mL, clear, yellow
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C29H29N7O2/c1-20-17-24(11-12-25(20)34-29-31-15-13-26(35-29)22-8-5-14-30-19-22)33-28(38)21-7-4-9-23(18-21)32-27(37)10-6-16-36(2)3/h4-15,17-19H,16H2,1-3H3,(H,32,37)(H,33,38)(H,31,34,35)/b10-6+
• chave InChI: GJFCSAPFHAXMSF-UXBLZVDNSA-N

Descrição

Descrição geral

A cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC₅₀ = 4.67 nM, 18.7 nM, 980 pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys¹¹⁶ in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC₅₀ = 486 nM in HeLa cells; 338 nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC₅₀ = 92 nM for V559D and 56 nM for T670I) and RIOK2 (120 nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK.

Ações bioquímicas/fisiológicas

Primary Target
JNK1, JNK2, JNK3

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

Zhang, T., et al. 2011. Chem. Biol.19, 140

Informações legais

Licensed under pending patent from Dana-Farber Cancer Institute.

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable