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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₂₉H₂₉N₇O₂
• Numer CAS: 1410880-22-6
• Masa cząsteczkowa: 507.59
• Numer MDL: MFCD22124890
• Kod UNSPSC: 12352200

Właściwości

• Próba: ≥97% (HPLC)
• Postać: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: light yellow to yellow
• rozpuszczalność: DMSO: 100 mg/mL, clear, yellow
• temp. przechowywania: 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+
• Klucz InChI: GJFCSAPFHAXMSF-UXBLZVDNSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Primary Target
JNK1, JNK2, JNK3

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

Licensed under pending patent from Dana-Farber Cancer Institute.

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable